Curriculum Vitae - UM College of Pharmacy



SCOTT D. LARSEN, Ph.D.PROFESSIONAL EXPERIENCEFibrosIX, Inc., East Lansing, MIVice President of Chemistry2018 - presentUniversity of Michigan, Ann Arbor, MIResearch Professor of Medicinal Chemistry – College of Pharmacy2007 - present Joseph Burckhalter Collegiate Research Professor2014 - 2019Director of Vahlteich Medicinal Chemistry Core2012 - 2019 Co-Director of Vahlteich Medicinal Chemistry Core2007 - 2012Pfizer, Inc., Ann Arbor, MI Research Fellow – Cardiovascular Chemistry2003 - 2007Pharmacia / Pharmacia & Upjohn / The Upjohn Co., Kalamazoo, MIAssociate Director and Fellow – Medicinal Chemistry2002 - 2003Senior Research Advisor – Medicinal Chemistry2001 - 2002Senior Scientist – Combinatorial and Medicinal Chemistry1997 - 2001Senior Research Scientist – Medicinal Chemistry 1992 - 1997Research Scientist – Metabolic Diseases 1988 - 1992Scientist – Atherosclerosis and Thrombosis1985 - 1988EDUCATIONPostdoctoral Research, Indiana University 1984-1985Advisor: Paul GriecoDevelopment of novel iminium Diels-Alder cycloadditionsPh.D. Organic Chemistry, University of Wisconsin-Madison1983Thesis Advisor: Edwin VedejsThesis Title: Macrocyclic Pyrrolizidine Alkaloids: The Total Synthesis of d,l-Fulvine and d,l-CrispatineB.S. Chemistry (summa cum laude), Alma College, Alma, MI1979HONORS AND AWARDSUM Collegiate Research Professor Award, 2014Pfizer Achievement Award, 2007Charter Member of the Pharmacia Fellows, 2001Pharmacia & Upjohn Special Recognition Awards 1998, 2000ACS Outstanding Undergraduate Chemistry Student Award, Alma College 1979Phi Sigma Pi Honor Society, 1978 (converted to Alma College Phi Beta Kappa chapter in 1979)TEACHING EXPERIENCEGraduate Students Mentored (degree, date, thesis title, initial postgraduate position attained)Chris George (MS, Sep 2009, “CNS-Permeable Inhibitors of Glucosylceramide Synthase”, chemist at Ascend Performance Materials)Jessica Bell (PhD, Aug 2012, “Novel Modulators of Rho Transcriptional Signaling in Cancer”, Assistant Professor of Chemistry at Northern Michigan University)Bryan Yestrepsky (PhD, Aug 2013, “Development of a Novel Class of Multifunctional Virulence-Attenuating Antibiotics”, ACS postdoctoral fellow with Paul Hergenrother at University of Illinois)Kyle Bolduc (PhD, Aug 2013, “Synthetic and Biocatalytic Methods for the Chemoenzymatic Production of Cryptophycin Analogs”, postdoc at Wolfe Labs)Janice Sindac (PhD, Aug 2014, “Development of Small Molecule Replication Inhibitors Against Western Equine Encephalitis Virus”, scientist at Tetra Discovery Partners, Kalamazoo, MI)Scott Barraza (PhD, Aug 2014, “Development of Novel Small Molecule Inhibitors of Neurotropic Alphavirus Replication”, postdoc with Scott Denmark at University of Illinois)Helen Waldschmidt (PhD, May 2017, “Development, Synthesis, and Characterization of G Protein-Coupled Receptor Kinase Inhibitors Using Structure Based Drug Design for the Advancement of Heart Failure Therapeutics”, postdoc with Bill Roush at Scripps FL)Jeff Zwicker (PhD, Aug 2018, “Development of CNS Penetrant Inhibitors of Toxoplasma Gondii Cathepsin L”, scientist at PharmAgra)Brandt Huddle (PhD, Aug 2018, “Development of Cancer-Stem-Cell Targeting Pan-Aldehyde Dehydrogenase Inhibitors as an Adjunct to Chemotherapy in the Treatment of Ovarian Cancer”, research associate at Tri-Institutional Therapeutics Discovery Institute, NYC)Dylan Kahl (PhD, Dec 2018, “Target Identification for and Optimization of Two Novel Series of Rho-mediated Gene Transcription Inhibitors with Anti-Fibrotic Properties”, scientific advisor at WSGR Legal Services)Dissertation Committees (year completed)Jiangwei Yao, Medicinal Chemistry (2010)Asako Kubota, Chemistry (2012)Elizabeth Girnys, Medicinal Chemistry (2012)Lauren Dixon Mishra, Medicinal Chemistry (2013)Solymar Negretti, Medicinal Chemistry (2013)Todd Eckroat, Medicinal Chemistry (2013)Xu Ran, Medicinal Chemistry (2014)Andrew Haak, Pharmacology (2014)Aubrie Harland, Medicinal Chemistry (2016)Aaron Bender, Medicinal Chemistry (2016)Zapporah Young, Medicinal Chemistry (2016)Carrie Johnson, ChemBio (2017)Megan Stewart, Medicinal Chemistry (2017)Tyler Beyett, ChemBio (2018)Jennifer Schmidt, Medicinal Chemistry (2018)Allie Sowa, Medicinal Chemistry (2018)Erin Gallagher, Medicinal Chemistry (2018)Anthony Nastase, Medicinal Chemistry (2018)Lindsey Drake, Medicinal Chemistry (2019)Amy Fraley, Medicinal Chemistry (2019)Deanna Montgomery, Medicinal Chemistry (2019) Sean Henry, Medicinal Chemistry (2019)Classes TaughtMedChem 740/741 “Preparing and Defending an Original Research Grant Proposal” (University of Michigan, 2017 - 2019)Course coordinatorMedChem 535 “Principles of Drug Design” (University of Michigan, 2017, 2019)Creator and coordinator of courseAdded to core med chem graduate curriculum 2017Proctored and scored drug development case history team presentationsMedChem 533 “Strategies in Drug Development” (University of Michigan, 2015)Creator and coordinator of course6 lectures (lead selection, chirality, conformational restriction, drug metabolism, drug development case history)Proctored and scored drug development case history team presentationsMedChem 532 “Bioorganic Principles of Medicinal Chemistry” (University of Michigan, 2007-2015, annual)Coordinator of course 2012-20156 lectures (introduction and drug metabolism)MedChem 635 “Principles of Drug Design” (University of Michigan, 2008, 2011)Creator and coordinator of course7 lectures (drug metabolism, lead selection, chirality, conformational restriction, drug development case histories)PharmD Investigations Review Committee (2009-2012)SUCCESSFUL EXTRAMURAL GRANT FUNDING (as Key Personnel)R01 CA238315-01(Buckanovich, PI)5/1/20-4/30/25“ALDH Inhibition as Modulator of Tumor Immunobiology”R21 GM134285-01(Trievel, PI)7/1/19-6/30/20“Unnatural Amino Acid Chemistry for Lysine Methyltransferase Substrate Discovery”R01 DK120623-01(Sexton, PI)4/1/19-1/31/22“Small molecules for expansion of islet beta-cell mass in diabetes”R33 AI127492-01(Larsen, Carruthers MPI)12/1/18-11/30/21“Rational design of CNS-permeable cathepsin L inhibitors for treatment of chronic toxoplasmosis”W81XWH1810587 (DoD)(Sandkvist, PI)9/1/18-8/31/21“Acinetobacter baumannii, Type II Secretion, and Therapeutic Targeting”R43 CA235823-01(Varnum, PI)9/1/18-4/30/19“Demonstrating the feasibility of CCG-257081 as a preventive therapy to inhibit bleomycin-induced lung fibrosis in mice”Harrington Discovery Institute(Shayman, PI)4/1/18-3/31/20“Brain penetrant glucosylceramide synthase inhibitors for the treatment of CNS based glycosphingolipidoses”R01 CA214567-01(Larsen, Buckanovich MPI)4/1/17-3/31/20“Isozyme-selective ALDH Inhibitors for Sensitizing Ovarian Cancer Stem-like Cells to Chemotherapy”R21 AI127492-01(Larsen, Carruthers MPI)12/1/16-11/30/18“Rational design of CNS-permeable cathepsin L inhibitors for treatment of chronic toxoplasmosis”R01 GM115459-01A1(Neubig, PI)4/1/16-3/31/19“Mechanisms of inhibitors of MRTF/SRF-regulated gene transcription”R01 AI116605-01A1(Abramovitch, PI)12/1/15-11/30/20“Mechanisms of Mycobacterium Tuberculosis pH-driven Adaptation”R01 HL071818-11A1(Tesmer, PI)7/1/15-6/30/17“Structure, function, and inhibition of G protein-coupled receptor kinases”UH2/UH3 NS092981-01(Larsen, Shayman MPI)7/1/15-6/30/18“The Development of Small Molecule Inhibitors for Gaucher Disease Type 3”R21 AI111182-01(Trievel, PI)9/1/14-8/31/16“Homocitrate Synthase Inhibitors as Novel Antifungal Agents for Aspergillus”R01 AR066049-01(Larsen, PI)5/1/14-4/30/17“Inhibition of the Rho/MRTF/SRF pathway as a new treatment for systemic sclerosis”R43 HL120441 (Baragi, PI)8/15/13-8/28/14“Selective MRTF/SRF-Transcription Inhibitors: Novel Anti-Fibrotics”R43 AR065314(Pape, PI)8/1/13-7/31/14“Targeted Small Molecule Medicinal Chemistry for Myotonic Dystrophy”R01 CA174667(Paczesny, PI)4/1/13-3/31/16“High throughput screening (HTS) to discover graft-versus-host disease inhibitors”R01 HD076004(Larsen, Shayman MPI)4/1/13-3/31/16“Novel Probes for Studying Treatment of CNS-based Lysosomal Storage Diseases”P50 GM103297 (Telenitsky, PI)9/17/12-8/31/17“The Center for HIV RNA Studies (CRNA)”P30 CA046592(Wicha, PI)9/1/12-8/31/17“University of Michigan Cancer Center Support Grant”2 R01 GM078200-08(Rosania, PI)9/1/12-7/31/16“Chemical Address Tags: A Cheminformatic & Image Data Management and Analysis Plan - admin supplement”R21 AI096985-01-A1(Al-Hashimi, PI)8/1/12-7/31/14“Biological Activity of Lead Compounds Targeting HIV-1 TAR RNA”.R21 NS079633-01(Shayman, PI)8/1/12-7/31/14“In vivo proof of efficacy studies for a novel glucosylceramide synthase inhibitor with central nervous system activity”R01 AI089417 (Miller, PI)7/1/10-6/30/15“Novel Therapeutics for Neurotropic Alphaviruses”R01 GM078200-S1(Rosania, PI)7/1/10-8/31/12“Chemical Address Tags: A Cheminformatic & Image Data Management and Analysis Plant”R01 HL0270973 (Martens, PI)4/1/10-3/31/14“Trafficking and Regulation of Cardiovascular K+ Channels”R21 NS065492 01A1(Larsen, PI)9/30/09-11/30/11“Design of CNS-Permeable Agents for the Treatment of Lipid Storage Diseases”R43 DK083074-01A1 (Hilfinger, PI)4/1/09-3/31/10“Development of orally delivered, non-absorbable AT1 receptor antagonists for inflammatory bowel disease treatment”P01 HL057346 11A1(Ginsburg, PI)4/1/09-3/31/15“Molecular Genetics of Coagulation Disorders”KEY SCIENTIFIC ACCOMPLISHMENTSPharmacia/PfizerDesign and development of hepatoselective inhibitors of hydroxymethylglutaryl-Coenzyme A (HMG-CoA) reductase. Identification of three clinical candidates.Synthesis and development of novel aminoguanidine antidiabetic/antiobesity agents. Identification of one clinical candidate. Development of a novel class of inhibitors of AcylCoA:Cholesterol O-Acyltransferase (ACAT) with in vivo cholesterol-lowering activity.Design and synthesis of novel seco-oxysterol inhibitors of HMG-CoA reductase gene transcription.Design of peptidomimetic PTP1B inhibitors with submicromolar potency and cell activity through multiple parallel synthesis, enzyme-ligand co-crystallization, and structure-based design.Design and synthesis of potent, orally bioavailable non-nucleoside DNA polymerase inhibitors University of Michigan Vahlteich Medicinal Chemistry Core (VMCC) Design of the first glucosylceramide synthase inhibitor that successfully lowered brain glycosphingolipid levels in a mouse model of Sandhoff disease From a high throughput screening lead, developed inhibitors of neurotropic arboviral RNA replication with protective effects in mouse models of infection. This was the first example of a small molecule therapeutic that lengthens lifespan in a WEEV infection model.Development of inhibitors of Rho-mediated gene transcription that inhibit cancer cell migration and attenuate up-regulation of pro-fibrotic genes in cells from human scleroderma patients CCG-203971 and CCG-222740 significantly attenuate development of dermal, colonic, lung and ocular fibrosis in murine modelsDesign of an affinity probe that successfully isolated the unknown molecular target from cell lysates, confirmed by xray co-crystallography with two ligandsDevelopment of orally active analogs (e.g. CCG-257081)Structure-based design of highly potent and selective inhibitors of G protein-coupled receptor kinase 2 with activity at stimulating cardiomyocyte contraction and in vivo activity in a murine model of heart failure.Structure-based design of highly potent and isoform selective inhibitors of aldehyde dehydrogenase 1A that synergize with cisplatin at killing ovarian cancer stem cellsFrom 2009-2019 the VMCC collectively contributed to successful grant awards totaling over $45M to the University of Michigan or other external partners (including $9M to the VMCC) in direct costs.PHARMA PROJECT LEADERSHIP EXPERIENCECholesterol Absorption Inhibitors (2006-2007, Pfizer): Transitioned exploratory project to full Lead Development stage (9 chemists).Contributed to the design of biomarker and early clinical development plans.Managed external contract chemistry supportHMG-CoA Reductase Inhibitors (2003-2006, Pfizer):Led chemistry team of 10-23 chemists in design and synthesis of over 1800 compounds. Advanced three compounds through FIH.Assisted in preparation of INDs and design of early clinical development plans.Protein Tyrosine Phosphatase 1B (1997-1998, Pharmacia):Leader of international multidisciplinary team (15-20 scientists) working on the design and development of peptidomimetic inhibitors. Successfully identified compounds with cellular activity.Antihyperglycemic Compounds (1994-1998, Pharmacia):Chemistry team leader for two different projects developing novel antihyperglycemics.Advanced one compound into FIH (PNU-106817).CONSULTINGMetabolic Solutions Development Company, Kalamazoo, MI (2008-2013)PSTology (2019-present)PROFESSIONAL MEMBERSHIPSAmerican Chemical Society (1985 – present)PROFESSIONAL SERVICEACS Medicinal Chemistry Division Long Range Planning Committee (2005 – 2007)NIH Special Emphasis Panel for NIH/NIDA RFA “Pharmacological Development of Treatment Agents and Formulations for Tobacco Dependence” (STTR R41), March 18, 2011.NIH NCATS TRND Contract Reviewer (ZTR1 DPI-3), February 28-March 1, 2013NIH NINDS NSD-A Study Section, February 22-23, 2016PUBLICATIONSInternal:Eighty-eight full Technical Reports at Upjohn/Pharmacia (1985-2003)External: Vedejs, E., Larsen, S.D. "Total Synthesis of d,lFulvine and d,lCrispatine," J. Am. Chem. Soc. 1984, 106, 3030-2. Vedejs, E., Larsen, S., West, F.G "Nonstabilized Imidate Ylides by the Desilylation Method: A Route to the Pyrrolizidine Alkaloids Retronecine and Indicine," J. Org. Chem. 1985, 50, 2170-4. Vedejs, E., Larsen, S. "Hydroxylation of Enolates with oxodiperoxymolybdenum(pyridine)(hexamethylphosphoric triamide): 1,7,7Trimethyl3hydroxybicyclo[2.2.1]heptan2one," Org. Synth. 1985, 64, 127. Larsen, S.D., Grieco, P.A. "Aza DielsAlder Reactions in Aqueous Solution: Cyclocondensation of Dienes with Simple Iminium Salts Generated under Mannich Conditions," J. Am. Chem. Soc. 1985, 107, 1768-9. Grieco, P.A., Larsen, S.D., Fobare, W.F. "Aza DielsAlder Reactions in Water: Cyclocondensation of CAcyl Iminium Ions with Cyclopentadiene," Tetrahedron Lett. 1986, 27, 1975-8. Larsen, S.D., Grieco, P.A., Fobare, W.F. "Reactions of Allylsilanes with Simple Iminium Salts in Water: A Facile Route to Piperidines via an Aminomethano DesilylationCyclization Process," J. Am. Chem. Soc. 1986, 108, 3512-13. Grieco, P.A., Larsen, S.D. "An Intramolecular Immonium Ion Variation of the DielsAlder Reaction: Synthesis of (±)Dihydrocannivonine," J. Org. Chem. 1986, 51, 3553-5. Vedejs, E., Ahmad, S., Larsen, S.D., Westwood, S. "Synthesis of Monocrotaline by Nucleophilic Macrolactonization," J. Org. Chem. 1987, 52, 3937-8. Larsen, S. D. "A Stereoselective Synthesis of Functionalized Cyclopentenes via BaseInduced Ring Contraction of Thiocarbonyl DielsAlder Adducts," J. Am. Chem. Soc. 1988, 110, 5932-4. Larsen, S. D., Martinborough, E. "Cycloaddition of ?Substituted Enones to a Bicyclic Sydnone: Observation of an Unexpectedly Facile Hydrocarbon Elimination," Tetrahedron Lett. 1989, 30, 4625-8.Grieco, P. A., Larsen, S. D. "Immonium Ion Based DielsAlder Reactions: N Benzyl2azanorbornene," Org. Synth. 1990, 68, 206-9. Larsen, S. D., Spilman, C. H., Bell, F. P., Dinh, D. M., Martinborough, E., Wilson, G. J. Synthesis and Hypocholesterolemic Activity of 6,7-Dihydro-4H-pyrazolo[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-diones, Novel Inhibitors of AcylCoA:Cholesterol O-Acyltransferase," J. Med. Chem. 1991, 34, 1721-7. Larsen, S.D., Spilman, C.H. "New Potential Therapies for the Treatment of Atherosclerosis," Ann. Rpts. Med. Chem. 1993, 28, 217-26. Larsen, S.D.; Spilman, C.H.; Yagi, Y.; Dinh, D.M.; Hart, K.L.; Hess, G.F. "Design and Synthesis of Seco-Oxysterols Analogs as Potential Inhibitors of 3-Hydroxy-3-methylglutaryl-Coenzyme A (HMG-CoA) Reductase Gene Transcription", J. Med. Chem 1994, 37, 2343-51. Larsen, S.D. "Regulators of 3-Hydroxy-3-methylglutaryl Coenzyme A Synthesis and Degradation", Drugs of the Future 1995, 20, 919-27. Larsen, S.D.; Fisher, P.V.; Libby, B.E.; Jensen, R.M.; Mizsak, S.A., Watt, W.; Ronk, W.R.; Hill, S.T. "Cyclopentene Synthesis from 1,3-Dienes via Base-Induced Ring Contraction of 3,6-Dihydro-2H-thiopyrans: Studies on Diastereoselection and Mechanism", J. Org. Chem. 1996, 61, 4725-38. Yagi, Y.; Bevis, D.J.; Hart, K.L.; Hess, G.F.; Dinh, D.M.; Keiser, B.J.; Larsen, S.D.; Spilman, C.H. "Screening for Inhibitors of HMG-CoA Reductase Promoter in HepG2: Identification of Four Non-Oxysterol Inhibitors", Drug Dev. Res. 1997, 40, 41-47. May, P.D.; Larsen, S.D. "Preparation of Novel 6-substituted-4-hydroxy-2-pyrone-3-carboxamides and esters via Palladium Catalyzed Cross Coupling Methodology", Synlett 1997, 895-6. Larsen, S.D. "Novel Parham-type Cycloacylations of 1H-Pyrazole-1-alkanoic Acids", Synlett 1997, 1013-14. Larsen, S.D.; Connell, M.A.; Cudahy, M.M.; Evans, B.R.; May, P.D.; Meglasson, M.D.; O'Sullivan, T.J.; Schostarez, H.J.; Sih, J.C.; Stevens, F.C.; Tanis, S.P.; Tegley, C.M.; Tucker, J.A.; Vaillancourt, V.A.; Vidmar, T.J.; Watt, W.; Yu, J.H. “Synthesis and Biological Activity of Analogues of the Antidiabetic/Antiobesity Agent 3-Guanidinopropionic Acid: Discovery of a Novel Aminoguanidinoacetic Acid Antidiabetic Agent”, J. Med. Chem. 2001, 44, 1217-30. Vaillancourt, V.A.; Larsen, S.D.; Tanis, S.P.; Burr, J.E.; Connell, M.A.; Cudahy, M.M.; Evans, B.R.; Fisher, P.V.; May, P.D.; Meglasson, M.D.; Robinson, D.R.; Stevens, F.C.; Vidmar, T.J.; Yu, J.H.; Tucker, J.A. “Synthesis and Biological Activity of Aminoguanidine and Diaminoguanidine Analogs of the Antidiabetic/Antiobesity Agent 3-Guanidinopropionic Acid”, J. Med. Chem. 2001, 44, 1231-48. Bleasdale, J.E.; Ogg, D.; Palazuk, B.J.; Jacob, C.S.; Swanson, M.L.; Wang, W.-Y.; Thompson, D.P.; Conradi, R.A.; Mathews, W.R.; Laborde, A.L.; Stuchley, C.J.; Heijbel, A.; Bergdahl, K.; Bannow, C.A.; Smith, C.W.; Liljebris, C.; Schostarez, H.J.; May, P.D.; Stevens, F.C.; Larsen, S.D. "Small Molecule Peptidomimetics Containing a Novel Phosphotyrosine Bioisostere Inhibit Protein Tyrosine Phosphatase 1B (PTP1B) and Augment Insulin Action", Biochemistry 2001, 40, 5642-54. Larsen, S.D.; DiPaolo, B.A. “Traceless Solid-Phase Synthesis of 1,2,4-Triazoles Using a Novel Amine Resin”, Org. Lett. 2001, 3, 3341-44.Larsen, S.D.; Barf, T.J.; Liljebris, C.; May, P.D.; Ogg, D.; O'Sullivan, T.J.; Palazuk, B.J.; Schostarez, H.J.; Stevens, F.C.; Bleasdale, J.E. "Synthesis and Biological Activity of a Novel Class of Small Molecular Weight Peptidomimetic Competitive Inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B)", J. Med. Chem. 2002, 45, 598-622.Liljebris, C.; Larsen, S.D.; Ogg, D.; Palazuk, B.J.; Bleasdale, J.E. “Investigation of Potential Bioisosteric Replacements for the Carboxyl Groups of Peptidomimetic Inhibitors of Protein Tyrosine Phosphatase 1B: Identification of a Tetrazole-Containing Inhibitor with Cellular Activity”, J. Med. Chem. 2002, 45, 1785-98.Larsen, S.D.; Stevens, F.C.; Lindberg, T.J.; Bodnar, P.M.; O’Sullivan, T.J.; Schostarez, H.J.; Palazuk, B.J.; Bleasdale, J.E. “Modification of the N-Terminus of Peptidomimetic Protein Tyrosine Phosphatase (PTP1B) Inhibitors: Identification of Analogs with Cellular Activity”, Bioorg. Med. Chem. Lett. 2003, 13, 971-75.Larsen, S.D.; Stachew, C.F.; Clare, P.M.; Cubbage, J.W.; Leach, K.L. “A Catch-and-Release Strategy for the Combinatorial Synthesis of 4-Acylamino-1,3-thiazoles as Potential cdk5 Inhibitors”, Bioorg. Med. Chem. Lett. 2003, 13, 3491-5.Larsen, S.D.; Hester, M.R.; Ruble, J. C.; Kamilar, G.M.; Romero, D.L.; Melchior, E.P.; Sweeney, M.T.; Marotti, K.R. “Discovery and Initial Development of a Novel Class of Antibacterials: Inhibitors of S. aureus Transcription/Translation”, Bioorg. Med. Chem. Lett 2006, 16, 6173-77.Larsen, S.D.; Zhang, Z.; DiPaolo, B.A..; Hageman, T.A.; Hopkins, M.L.; Oien, N.L.; Rohrer, D.C.; Rush, B.D.; Schwende, F.J.; Stefanski, K.J.; Wieber, J.L.; Wilkinson, K.F.; Zamora, K.M. ; Wathen, J.L.; Brideau, R.J “7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: Synthesis and Biological Activity of a New Class of Highly Potent Inhibitors of Human Cytomegalovirus DNA Polymerase”, Bioorg. Med. Chem. Lett. 2007, 17, 3840-44.Bratton, L.D.; Auerbach, B.; Choi, C.; Dillon, L.; Hanselman, J.C.; Larsen, S.D.; Lu, G.; Olsen, K.; Pfefferkorn, J.A.; Robertson, A.; Sekerke, C.; Trivedi, B.K.; Unangst, P.C. “Discovery of Pyrrole-based Hepatoselective Ligands as Potent Inhibitors of HMG-CoA Reductase”, Bioorg. Med. Chem. 2007, 15, 5576-89.Pfefferkorn, J.A.; Bowles, D; Kissel, W.; Boyles, D.; Choi, C.; Larsen, S.D.; Song, Y.; Sun, K.-L.; Miller, S.; Trivedi, B.K. “Development of a Practical Synthesis of Novel Pyrrole-Based HMG-CoA Reductase Inhibitors”, Tetrahedron 2007, 63, 8124-34.Pfefferkorn, J.A.; Choi, C.; Song, Y.; Trivedi, B.K.?; Larsen, S.D.?; Askew, V.; Dillon, L.; Hanselman, J.C.; Lin, Z.; Lu, G.; Robertson, A.; Sekerke, C.; Auerbach, B.; Pavlovsky, A.; Harris, M.S.; Bainbridge, G.; Caspers, N. “Design and Synthesis of Novel, Conformationally Restricted HMG-CoA Reductase Inhibitors”, Bioorg. Med. Chem. Lett. 2007, 17, 4531-37.Larsen, S.D.; Poel, T.-J.; Filipski, K.J.; Kohrt, J.T.; Pfefferkorn, J.A.; Sorenson, R.J.; Askew, V.; Dillon, L.; Hanselman, J.C.; Lu, G.H.; Robertson, A.; Sekerke, C.; Auerbach, B.J. “Pyrazole Inhibitors of HMG-CoA Reductase: An Attempt to Dramatically Reduce Synthetic Complexity through Minimal Analog Re-design”, Bioorg. Med. Chem. Lett. 2007, 17, 5567-72.Pfefferkorn, J.A.; Song, Y.; Sun, K.-L.; Miller, S.R.; Trivedi, B.K.; Choi, C.; Sorenson, R.; Bratton, L.D.; Unangst, P.C.; Larsen, S.D.; Poel, T.-J.; Cheng, X.-M.; Lee, C.; Erasga, N.; Auerbach, B.; Askew, V.; Dillon, L.; Hanselman, J.C.; Lin, Z.; Lu, G.; Robertson, A.; Olsen, K.; Mertz, T.; Sekerke, C.; Pavlovsky, A.; Harris, M.S.; Bainbridge, G.; Caspers, N.; Chen, H.; Eberstadt. M. “Design and Synthesis of Hepatoselective, Pyrrole-Based HMG-CoA Reductase Inhibitors”, Bioorg. Med. Chem. Lett. 2007, 17, 4538-44.Pfefferkorn, J.A.; Larsen, S.D.; Van Huis, C.; Sorenson, R.; Barton, T.; Winters, T.; Auerbach, B.; Wu, C.; Wolfram, T.J.; Cai, H.; Welch, K.; Esmaiel, N.; Davis, J.; Bousley, R.; Olsen, K.; Bak Mueller, S.; Mertz, T. “Substituted Oxazolidinones as Novel NPC1L1 Ligands for The Inhibition of Cholesterol Absorption”, Bioorg. Med. Chem. Lett. 2008, 18, 546-53. Pfefferkorn, J.A.; Choi, C.; Larsen, S.D.; Auerbach, B.; Hutchings, R.; Park, W.; Askew, V.; Dillon, L.; Hanselman, J.C.; Lin, Z.; Lu, G.H.; Robertson, A.; Sekerke, C.; Harris, M.S.; Pavlovsky, A.; Bainbridge, G.; Caspers, N.; Kowala, M.; Tait, B.D. “Substituted Pyrazoles as Hepatoselective HMG-CoA Reductase Inhibitors: Discovery of PF-3052334 as a Candidate for the Treatment of Hypercholesterolemia”, J. Med. Chem. 2008, 51, 31-45.Park, W.K.C.; Kennedy, R.M.; Larsen, S.D.; Miller, S.; Roth, B.D.; Song, Y.; Steinbaugh, B.A.; Sun, K.; Tait, B.D; Kowala, M.C.; Trivedi, B.K.; Auerbach, B.; Askew, V.; Dillon, L.; Hanselman, J.C.; Lin, Z; Lu, G.H.; Robertson, A.; Sekerke, C. “Hepatoselectivity of Statins: Design and Synthesis of 4-Sulfamoyl Pyrroles as HMG-CoA Reductase Inhibitors”, Bioorg. Med. Chem. Lett. 2008, 18, 1151-56.Sarver, R.W.; Bills, E.; Bolton, G.; Bratton, L.D.; Caspers, N.L.; Dunbar, J.B.; Harris, M.S.; Hutchings, R.H.; Kennedy, R.M.; Larsen, S.D.; Pavlovsky, A.; Pfefferkorn, J.A.; Bainbridge, G. “Thermodynamic and Structure Guided Design of Statin-Based Inhibitors of 3-Hydroxy-3-methylglutaryl Coenzyme A Reductase” J. Med. Chem. 2008, 51, 3804-13.Bowles, D.M.; Bolton, G.L.; Boyles, D.C.; Curran, T.T.; Hutchings, R.H.; Larsen, S.D.; Miller, J.M.; Park, W.K.C.; Ritsema, K.G.; Schineman, D.C.; Tamm, M. “Preparation of a HMG-CoA Reductase Inhibitor via an Optimized Imidazole-Forming Condensation Reaction”, Org. Proc. Res. Dev., 2008, 12, 1183-87.Peng, W.; Peltier, D.C.; Larsen, M.J.; Kirchhoff, P.D.; Larsen, S.D.; Neubig, R.R.; Miller, D.J. “The Identification of Thieno[3,2-b]pyrrole Derivatives as Novel Small Molecule Inhibitors of Neurotropic Alphaviruses”, J. Infect. Diseases 2009, 199, 950-57.Evelyn, C.R.; Bell, J.L., Ryu, J.G.; Wade, S.M., Kocab A., Harzdorf, N.L., Showalter, H.D.H., Neubig, R.R., Larsen, S.D. “Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423”, Bioorg. Med. Chem. Lett 2010, 20, 665-72.Okawada, M.; Koga, H.; Larsen, S.D.; Showalter, H.D.; Turbiak, A.J..; Lucas, P.; Xiaohong, J.; Lipka, E.; Hilfinger, J.; Kim, J.S.; Teitelbaum, D.H. “Use of Enterally-Delivered Angiotensin II Type IA Receptor Antagonists to Reduce the Severity of Colitis”, Dig. Dis. Sci. 2011, 56, 2553-65. Yep, A.; Sorenson, R.J.; Wilson, M.W.; Showalter, H.D.H.; Larsen, S.D.; Keller, P.R.; Woodard, R.W. “Enediol mimics as inhibitors of the D-arabinose 5-phosphate isomerase (KdsD) from Francisella tularensis”, Bioorg. Med. Chem. Lett. 2011, 21, 2679-82. Pfefferkorn, J.A.; Litchfield, J.; Hutchings, R.; Cheng, X.-M.; Larsen, S.D.; Auerbach, B.A.; Bush, M.R.; Lee, C.; Erasga, N.; Bowles, D.; Boyles, D.C.; Lu, G.; Sekerke, C.; Askew, V.; Hanselman, J.; Dillon, L.; Lin, Z.; Robertson, A.; Olsen, K.; Boustany, C.; Atkinson, K.; Goosen, T.; Sahasrabudhe, V.; Chupka, J.; Duignan, D.B.; Feng, B.; Scialis, R.; Kimoto, E.; Bi, Y.-A.; Lai, Y.; El-Kattan, A.; Bakker-Arkema, R.; Barclay, P.; Kindt, E.; Le, V.; Mandema, J.W.; Milad, M.; Tait, B.D.; Kennedy, R.; Trivedi, B.K.; Kowala, M. “Discovery of Novel Hepatoselective HMG-CoA Reductase Inhibitors for Treating Hypercholesterolemia: A Bench-to-Bedside Case Study on Tissue Selective Drug Distribution”, Bioorg. Med. Chem. Lett. 2011, 21, 2725-31. Fribley, A.; Cruz, P.; Miller, J.; Callaghan, M.; Cai, P.; Narula, N.; Neubig, R.; Showalter, H.; Larsen, S.; Kirchhoff, P.; Larsen, M.; Burr, D.; Schultz, P.; Jacob, R.; Tamayo-Castillo, G.; Sherman, D.; Ron, D.; Kaufman, R. “Complementary Cell-based High Throughput Screens Identify Novel Modulators of the Unfolded Protein Response”, J. Biomol. Screening 2011, 16, 825-35.Puliyappadamba, T; Wu, W.; Polin, L.; Kilkuskie, R.; FinleyR.; Larsen, S.D.; Levi, E.; Miller, F.R.; Wali, A.; Rishi, A.K. “Antagonists of Anaphase Promoting Complex (APC)-2-Cell cycle and Apoptosis Regulatory Protein (CARP)-1 interaction are novel regulators of cell growth and apoptosis”, J. Biol. Chem. 2011, 286, 38000-17. Larsen, S.D.; Wilson, M.W.; Abe, A.; Shu, L.; George, C.H.; Kirchhoff, P.; Showalter, H.W.; Xiang, J.; Keep, R.F.; Shayman, J.A. “Property-based design of a substrate-based gluocosylceramide synthase inhibitor that reduces glucosylceramide levels in the central nervous system”, J. Lipid Res. 2012, 53, 282-91.This article was selected for publication in Global Medical Discovery.Sun, H.; Xu, Y.; Sitkiewicz, I.; Ma, Y.; Wang, X.; Yestrepsky, B.D.; Huang, Y.; Lapadatscu, M.C.; Larsen, M.J.; Larsen, S.D.; Musser, J.M.; Ginsburg, D. “Inhibitor of streptokinase gene expression improves survival after group A streptococcus infection in mice”, Proc. Nat. Acad. Sci. 2012, 109, 3469-74.Sindac, J.S.; Yestrepsky, B.D.; Barraza, S.J.; Bolduc, K.L.; Blakely, P.K.; Keep, R.F.; Irani, D.N.; Miller, D.J.; Larsen, S.D. “Novel Inhibitors of Neurotropic Alphavirus Replication That Improve Host Survival in a Mouse Model of Acute Viral Encephalitis”, J Med Chem 2012, 55, 3535-45.Wang, Y.; Cesena, T.I.; Ohnishi, Y.; Burger-Caplan, R.; Lam, V.; Kirchhoff, P.D.; Larsen, S.D.; Larsen, M.J.; Nestler, E.J.; Rudenko, G. “Small molecule screening identifies regulators of the transcription factor deltaFosB”, ACS Chem. Neuroscience 2012, 3, 546-56.Bolduc, K.L.; Larsen, S.D.; Sherman, D.H. “Efficient, Divergent Synthesis of Cryptophycin Unit A Analogues”, JCS Chem. Comm. 2012, 48, 6414-16.Jacob, R.T.; Larsen, M.J.; Larsen, S.D.; Kirchhoff, P.D.; Sherman, D.H.; Neubig, R.R. “MScreen: An Integrated Compound Management and High Throughput Screening (HTS) Data Storage and Analysis System”, J. Biomol. Screening 2012, 17, 1080-87.Ma, Y.; Xu, Y.; Yestrepsky, B.D.; Sorenson, R.J.; Chen, M.; Larsen, S.D.; Sun, H. “Novel inhibitors of Staphylococcus aureus virulence gene expression and biofilm formation”, PLoS ONE 2012, 7, e47225.Yestrepsky, B.D.; Xu, Y.; Sorenson, R.J.; Wilson, M.W.; Ryu, J.; Rajaswaran, W.; Breen, M.E.; Tsume, Y.; Zhang, W.; Li, X.; Sun, D.; Sun, H.; Larsen, S.D. “Novel Inhibitors of Bacterial Virulence: Development of 5,6-Dihydrobenzo[h]quinazoline-4(3H)-ones for the Inhibition of Group A Streptococcal Streptokinase Expression”, Bioorg. Med. Chem. 2013, 21, 1880-97.Arthur, J.R.; Wilson, M.W.; Larsen, S.D.; Shayman, J.A.; Seyfried, T.N. “Ethylenedioxy-PIP2 oxalate reduces ganglioside storage in brain and liver of mice with Sandhoff disease”, Neurochem. Res. 2013, 38, 866-75.Bell, J.L.; Haak, A.J.; Wade, S.M.; Sun, Y.; Neubig, R.R.; Larsen, S.D. “Design and synthesis of tag-free photoprobes for the identification of the molecular target for CCG-1423, a novel inhibitor of the Rho/MKL1/SRF signaling pathway”, Beilstein J. Org. Chem. 2013, 9, 966-73.Bell, J.L.; Haak, A.J.; Wade, S.M., Kirchhoff, P.D.; Neubig, R.R.; Larsen, S.D. “Optimization of Novel Nipecotic Bis(amide) Inhibitors of the Rho/MKL1/SRF Transcriptional Pathway as Potential Anti-metastasis Agents”, Bioorg. Med. Chem. Lett. 2013, 23, 3826-32.Sindac, J.A.; Barraza, S.J.; Dobry, C.J.; Xiang, J.; Blakely, P.K.; Irani, D.N.; Keep, R.F.; Miller, D.J.; Larsen, S.D. “Optimization of Novel Indole-2-carboxamide Inhibitors of Neurotropic Alphavirus Replication”, J. Med. Chem. 2013, 56, 9222-41.Johnson, L.A.; Rodansky, E.; Haak, A.; Larsen, S.D.; Neubig, R.R.; Higgins, P.D.R. “Novel Rho/MRTF-A Inhibitors Block Matrix-stiffness and TGF?-Induced Fibrogenesis in Human Colonic Myofibroblasts”, Inflamm. Bowel Dis. 2014, 20, 154-65.Lundquist, M.R.; Storaska, A.; Liu, T.-C.; Larsen, S.D.; Evans, T.; Neubig, R.R.; Jaffrey, S.R. “Redox modification of nuclear actin by MICAL-2 regulates SRF signaling”, Cell 2014, 156, 563-76.Homan, K.T.; Wu, E.; Wilson, M.W.; Singh, P.; Larsen, S.D.; Tesmer, J.J.G. “Structural and Functional Analysis of G Protein-Coupled Receptor Kinase Inhibition by Paroxetine and a Rationally Designed Analog”, Mol. Pharmacol. 2014, 85, 237-48.Yestrepsky, B.D.; Kretz, C.; Xu, Y.; Holmes, A.; Sun, H.; Ginsburg, D.; Larsen, S.D. “Development of tag-free photoprobes for studies aimed at identifying the target of novel Group A Streptococcus antivirulence agents”, Bioorg. Med. Chem. Lett. 2014, 24, 1538-44.Larsen, M.J.; Larsen, S.D.; Fribley, A.; Grembecka, J.; Haak, A; Homan, K.; Mapp, A.; Nikolovska-Coleska, Z.; Stuckey, J.A.; Sun, D.; Sherman, D.H. “The Role of HTS in Drug Discovery at University of Michigan”, Combi. Chem. & High Throughput Screening 2014, 17, 210-30.Baez-Santos, Y.M.; Barraza, S.J.; Wilson, M.W.; Agius, M.P.; Mielech, A.; Davis, N.M.; Baker, S.C.; Larsen, S.D.; Mesecar, A.D. “X-Ray Structural and Biological Evaluation of a Series of Potent and Highly Selective Inhibitors of Human Coronavirus Papain Like-Proteases”, J. Med. Chem., 2014, 57, 2393-2412.Haak, A.; Tsou, P.-S.; Amin, M.A.; Ruth, J.H.; Campbell, P.; Fox, D.A.; Khanna, D.; Larsen, S.D.; Neubig, R.R. “Targeting the myofibroblast genetic switch: inhibitors of MRTF/SRF-regulated gene transcription prevent fibrosis in a murine model of skin injury”, J. Pharmacol. Exp. Ther. 2014, 349, 480-86.Shayman, J.A.; Larsen, S.D. “The Development and Use of Small Molecule Inhibitors of Glycosphingolipid Metabolism for the Treatment of Lysosomal Storage Disease”, J. Lipid Res. 2014, 55, 1215-25.Delekta, P.C.; Dobry, C.J.; Sindac, J.A.; Barraza, S.J.; Blakely, P.K.; Xiang, J.; Kirchhoff, P.D.; Keep, R.F.; Irani, D.N.; Larsen, S.D.; Miller, D.J. “Novel indole-2-carboxamide compounds are potent broad spectrum antivirals active against western equine encephalitis virus in vivo”, J. Virology 2014, 88, 11199-11214. Deng, X.; Agnihothram, S.; Mielech, A.M.; Nichols, D.B.; St. John, S.; Wilson, M.W.; Larsen, S.D.; Mesecar, A.D.; Lenschow, D.J.; Baric, R.; Baker, S.C. “A Chimeric Virus-Mouse Model System for Evaluating the Function and Inhibition of Papain-like Proteases of Emerging Coronaviruses”, J. Virology 2014, 88, 11825-33.Barraza, S.J.; Delekta, P.C.; Sindac, J.A.; Dobry, C.J.; Xiang, J.; Keep, R.F.; Miller, D.J.; Larsen,S.D. “Discovery of Anthranilamides as a Novel Class of Inhibitors of Neurotropic Alphavirus Replication”, Bioorg. Med. Chem 2015, 23, 1569-87.Sisson, T.H.; Ajayi, I.O.; Subbotina, N.; Dodi, A.E.; Rodansky, E.S.; Chibucos, L.N.; Kim, K.K.; Keshamouni, V.G.; White, E.S.; Zhou, Y.; Higgins, P.D.R.; Larsen, S.D.; Neubig, R.R.; Horowitz, J.C. “Inhibition of MRTF/SRF Signaling Decreases Lung Fibrosis and Promotes Mesenchymal Cell Apoptosis”, Am. J. Pathology, 2015, 185, 969-86.Min, K.A.; Rajeswaran, W.G.; Oldenbourg, R.; Harris, G.; Keswani, R.K.; Chiang, M.; Rzeczycki, P., Talattof, A.; Hafeez, M.; Horobin, R.W.; Larsen, S.D.; Stringer, K.A.; Rosania, G.R. “Massive Bioaccumulation and Self-Assembly of Phenazine Compounds in Live Cells”, Adv. Sci. 2015 2, 1500025.Homan, K.T.; Waldschmidt, H; Glukhova, A.; Cannavo, A.; Song, J.; Cheung, J.Y.; Koch, W.J.; Larsen, S.D.; Tesmer, J.J.G. “Crystal Structure of G Protein-Coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor “, J. Biol. Chem. 2015 290, 20649-59. This article was selected as a JBC Paper of the Week.Muthu, M.; Somagoni, J.; Cheriyan, V.T.; Munie, S.; Levi, E.; Ashour, A.E.; Alaa, E.B.; Alafeefy, A.M.; Sochacki, P.; Polin, L.A.; Reddy, K.B.; Larsen, S.D.; Singh, M.; Rishi, A.K. “Identification and testing of novel CARP-1 functional mimetic compounds as inhibitors of non-small cell lung and triple negative breast cancers”, J. Biomed. Nanotech. 2015 11, 1608-27.Waldschmidt, H.; Homan, K.; Cruz-Rodriguez, O.; Cato, M.; Waninger-Saroni, J.; Larimore, K.; Cannavo, A.; Song, J.; Cheung, J.; Koch, W.; Tesmer, J.; Larsen, S.D. “Structure-Based Design, Synthesis and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors”, J. Med. Chem. 2016 59, 3793-3807.Bolinger, M.; Ramshekar, A.; Waldschmidt, H.; Larsen, S.; Bewley, M.; Flanagan, J.; Antonetti, D. “Occludin S471 phosphorylation contributes to epithelial monolayer maturation”, Mol. Cell Biol. 2016 36, 2051-66.Beck, M.W.; Kerr, R.A.; Derrick, J.S.; Oh, S.B.; Cho, W.J.; Lee, S.J.C.; Tehrani, Z.A.; Suh, N.; Kim, S.; Ji, Y.; Larsen, S.D.; Kim, K.S.; Lee, J.-Y.; Ruotolo, B.T.; Lim, M.H. “Structure-mechanism-based engineering of chemical regulators targeting distinct pathological factors in Alzheimer’s disease”, Nat. Comm. 2016 7, 13115.Okawada, M.; Wilson, M.W.; Larsen, S.D.; Lipka, E.; Hillfinger, J.; Teitelbaum, D.H. “Blockade of the renin-angiotensin system prevents acute and immunologically relevant colitis in murine models”, Pediatr. Surg. Int. 2016, 32, 1103-14.Zheng, H.; Colvin, C.J.; Johnson, B.K.; Kirchhoff, P.; Wilson, M.; Jorgensen-Muga, K.; Larsen, S.D.; Abramovitch, R.B. “Inhibitors of Mycobacterium tuberculosis DosRST signaling and persistence”, Nat. Chem. Biol. 2016, 13, 218-25. Cheriyan, V.T; Muthu, M.; Sekhar, S.; Patel, K.; Larsen, S.D.; Polin, L.; Levi, E.; Singh, M.; Rishi, A.K. “CARP-1 functional mimetics are novel inhibitors of drug-resistant triple negative breast cancers”, Oncotarget 2016, 7, 73370-88.Johnson, L.; Rodansky, E.; Moons, D.; Larsen, S.; Neubig, R.; Higgins, P. “Optimization of intestinal fibrosis and survival in the mouse S. typhimurium model for anti-fibrotic drug discovery and pre-clinical applications”, “J. Crohn’s & Colitis, 2016, 11, 724-36.Haak, A.J.; Appleton, K.M.; Mathes, E.; Misek, S.; Ji, Y.; Wade, S.M.; Bell, J.L.; Rockwell, C.E.; Airik, M.; Krook, M.A.; Larsen, S.D.; Verhaegan, M.; Lawlor, E.R.; Neubig, R.R. “Pharmacological inhibition of Myocardin-related transcription factor pathway blocks lung metastases of RhoC overexpressing melanoma”, Mol. Canc. Ther. 2017, 16, 193-204.Yu-Wai-Man, C.; Spencer-Dene, B; Lee, R.M.H; Hutchings, K.; Lisabeth, E.M.; Treisman, R.; Bailly, M.; Larsen, S.D.; Neubig, R.R.; Khaw, P.T. “Local delivery of novel MRTF/SRF inhibitors prevents scar tissue formation in a preclinical model of fibrosis”, Sci. Rep. 2017, 7, 518.Hutchings, K.M.; Lisabeth, E.M.; Rajeswaran, W.; Wilson, M.W.; Sorenson, R.J.; Campbell, P.L.; Ruth, J.H.; Amin, A.; Tsou, P.-S.; Leipprandt, J.R.; Olson, S.R.; Wen, B.; Zhao, T.; Sun, D.; Khanna, D.; Fox, D.A.; Neubig, R.R.; Larsen, S.D. “Pharmacokinetic Optimization of CCG-203971: Novel Inhibitors of the Rho/MRTF/SRF Transcriptional Pathway as Potential Antifibrotic Therapeutics for Systemic Scleroderma”, Bioorg. Med. Chem. Lett. 2017, 27, 1744-49.Waldschmidt, H.V.; Homan, K.T.; Cato, M.C.; Cruz-Rodriguez, O.; Cannavo, A.; Wilson, M.W.; Song, J.; Cheung, J.Y.; Koch, W.J.; Tesmer, J.J.G.; Larsen, S.D. “Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine”, J. Med. Chem 2017, 60, 3052-69.Beck, M.W.; Derrick, J.S.; Suh, J.-M; Kim, M.; Korshavn, K.J.; Kerr, R.A.;.; Cho, W.J.; Larsen, S.D.; Kim, K.S.; Ruotolo, B.T.; Ramamoorthy, A.; Lim, M.H. “Minor structural variations of small molecules tune regulatory activities towards pathological factors in Alzheimer’s disease”, ChemMedChem 2017, 12, 1828-38.Bouley, R.; Waldschmidt, H.V.; Cato, C.; Cannovo, A.; Song, J.; Cheung, J.Y.; Yao, X.-Q.; Koch, W.J.; Larsen, S.D.; Tesmer, J.J.G. “Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Kinase 2 Inhibitors”, Mol. Pharm. 2017, 92, 707-17. Murashov, M. D; LaLone, V.; Rzeczycki, P. M.; Keswani, R.K.; Yoon, G.S.; Sud, S.; Rajeswaran, W.; Larsen, S.; Stringer, K.A.; Rosania, G.R. “The Physicochemical Basis of Clofazimine-Induced Skin Pigmentation”, J. Invest. Dermatol. 2018, 138, 697-703.Stoveken, H.M.; Larsen, S.D.; Smrcka, A.V.; Tall, G.G. “Gedunin- and Khivorin-Derivatives are Small Molecule Partial Agonists for Adhesion G protein Coupled Receptors GPR56 / ADGRG1 and GPR114 / ADGRG5”, Mol. Pharm. 2018, 93, 477-88.Zwicker, J.D.; Diaz, N.A.; Guerra, A.J.; Kirchhoff, P.D.; Wen, B.; Sun, D.; Carruthers, V.B.; Larsen, S.D. “Optimization of Dipeptidic Inhibitors of Cathepsin L for Toxoplasma gondii Selectivity and CNS Permeability”, Bioorg. Med. Chem. Lett. 2018, 28, 1972-80.Waldschmidt, H.V.; Bouley, R.; Kirchhoff, P.D.; Lee, P.H.; Tesmer, J.J.G.; Larsen, S.D. “Utilizing a Structure-Based Docking Approach to Develop Potent G Protein-Coupled Receptor Kinase (GRK) 2 and 5 Inhibitors”, Bioorg. Med. Chem. Lett. 2018, 28, 1507-15.Huddle, B.C.; Buchman, C.D.; Chtcherbinine, M.; Grimley, E.; Debnath, B.; Mehta, P.; Yang, K.; Morgan, C.A.; Li, S.; Felton, J.; Sun, D.; Mehta, G.; Neamati, N.; Buckanovich, R.J. Hurley, T.D.; Larsen, S.D. “Structure-Based Optimization of a Novel Class of Aldehyde Dehydrogenase 1A (ALDH1A) Subfamily-Selective Inhibitors as Potential Adjuncts to Ovarian Cancer Chemotherapy”, J. Med. Chem.2018, 61, 8754-73.Tanis, S.P.; Colca, J.R.; Parker, T.T.; Artman, G.D.; Larsen, S.D.; McDonald, W.; Gadwood, R.C.; Kletzien, R.F.; Zeller, J.B.; Lee, P.; Adams, W.J. “PPARγ-Sparing Thiazolidinediones as Insulin Sensitizers. Design, Synthesis and Selection of Compounds for Clinical Development”, Bioorg. Med. Chem. 2018, 26, 5870-84.Tagalkakis, A.D.; Madaan, S.; Larsen, S.D.; Neubig, R.R.; Khaw, P.T.; Yu-Wai-Man, C. “In vitro and in vivo evaluation of a sustained release nanocarrier-based formulation of MRTF/SRF inhibitors in conjunctival fibrosis”, J. Nanobiotech. 2018, 16, 97. Dumas, M.; Chen, G.-Y.; Kendrick, N.; Xu, G.; Larsen, S.D.; Jana, S.; Waterson, A.; Bauer, J.; Hancock, W.; Sulikowski, G.; Ohi, R. “Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes”, Bioorg. Med. Chem. Lett. 2019, 29, 148-54.Chefetz, I.; Yang, K.; Grimley, E.; Hong, L.; Vinogradova, E.; Suciu, R.; Cravatt, B.; Kovalencko, I.; Karnak, D.; Morgan, M.; Morgan, C.; Chtcherbinine M.; Buchman, C.; Huddle, B.; Barraza, S.; Morgan, M.; Lombard, D.; Romero, I.; Chiang, C.-Y.; Landen, C.; Hurley, T.; Barraza, S.; Huddle, B.; Larsen, S.D.; Bernstein K.A.; Yoon, E.; Lombard, D.B; Bild, A.; Mehta, G.; Romero, I.; Chiang, C.-Y.; Landen, C.;?Buckanovich, R.J. “A Pan-ALDH1A Inhibitor Induces Necroptosis in Ovarian Cancer Stem-Like Cells”, Cell Reports 2019, 26, 3061-75, e6. Gan, X.; Wilson, M.W.; Beyett, T.S.; Wen, B.; Sun, D.; Larsen, S.D.; Tesmer, J.J.G.; Saltiel, A.R.; Showalter, H.D. “Synthesis of deuterium-labeled amlexanox and its metabolic stability against mouse, rat and human microsomes”, J. Label Compd Radiopharm 2019, 62, 202-8.Lisabeth, E.M.; Kahl, D.; Gopallawa, I.; Haynes, S.E.; Misek, S.A.; Campbell, P.L.; Dexheimer, T.S.; Khanna, D.; Fox, D.A.; Jin, X.; Martin, B.R.; Larsen, S.D.; Neubig, R.R. “Identification of Pirin as a Molecular Target of the CCG-1423/CCG-203971 Series of Anti-Fibrotic and Anti-Metastatic Compounds”, ACS Pharmacol & Trans Science 2019, 2, 92-100.Kahl, D; Hutchings, K.M.; Lisabeth, E.M.; Haak, A.J.; Leipprandt, J.R.; Khanna, D.; Tsou, P.-S.; Campbell, P.L.; Fox, D.A.; Wen, B.; Sun, D.; Bailie, M.; Neubig, R.R.; Larsen, S.D. “5-Aryl-1,3,4-oxadiazol-2-ylthioalkanoic Acids: A Highly Potent New Class of Inhibitors of Rho/MRTF/SRF-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma”, J. Med. Chem. 2019, 62, 4350-69.Tanis, S.P.; Colca, J.R.; Parker, T.T.; Artman, G.D.; Larsen, S.D.; Gadwood, R.C.; Zeller, J.R. “The Development of Improved Syntheses of PPAR-Sparing, Insulin Sensitizing Thiazolidinedione-ketones”, Tet. Lett. 2019, 60, 150931.Rowlands, R.; Cato, M.; Waldschmidt, H.; Bouley, R.; Larsen, S.; Tesmer, J.; White, A. “Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors” ACS Med Chem Lett 2019, 10, 1628-34.Misek, S.A., Appleton, K.A.; Dexheimer, T.; Lisabeth, E.M.; Lo, R.S.; Larsen, S.D.; Gallo, K.A.; Neubig, R.R. “ Rho-mediated signaling promotes BRAF inhibitor resistance in de-differentiated melanoma cells”, Oncogene 2020, 39, 1466-83.Zwicker, J.D.; Smith, D.; Guerra, A.J.; Hitchens, J.R.; Haug, N.; Vander Roest, S.; Lee, P.; Wen, B.; Sun, D.; Wang, L.; Keep, R.F.; Xiang, J.; Carruthers, V.B.; Larsen, S.D. “Discovery and Optimization of Triazine Nitrile Inhibitors of Toxoplasma gondii Cathepsin L for the Treatment of Chronic Toxoplasmosis in the CNS”, ACS Chem. Neuroscience 2020, 11, 2450-63.Bouley, R.A.; Weinberg, Z.Y.; Waldschmidt, H.V.; Larsen, S.D.; Puthenveedu, M.A.; Tesmer, J.J.G. “A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the ?-Opioid Receptor”, Mol. Pharm. 2020, 97, 392-413.Wilson, M.W.; Shu, L.; Hinkovska-Galcheva, V.; Jin, Y.; Rajeswaran, W.; Abe, A.; Zhao, T.; Luo, R.; Wang, L.; Wen, B.; Liou, B.; Fannin, V.; Sun, D.; Sun, Y.; Shayman, J.A.; Larsen, S.D. “Optimization of Eliglustat-based Glucosylceramide Synthase Inhibitors as Substrate Reduction Therapy for Gaucher Disease Type 3”, ACS Chem. Neuroscience 2020, 11, 3464-73.Dechow, S.J.; Coulson, G.B.; Wilson, M.W.; Larsen, S.D.; Abramovitch, R.B. “AC2P20 selectively kills M. tuberculosis at acidic pH by depleting free thiols”, RSC Chem. Biol. submitted for publication.Huddle, B.C.; Grimley, E.; Chtcherbinine, M.; Buchman, C.D.; Debnath, B.; McGonigal, S.C.; Mao, S.; Li, S.; Felton, J.; Pan, S.; Wen, B.; Sun, D.; Neamati, N.; Buckanovich, R.J.; Hurley, T.D.; Larsen, S.D. “Development of 2,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of Aldehyde Dehydrogenase 1A (ALDH1A) as potential adjuncts to ovarian cancer chemotherapy”, Eur. J. Med. Chem. submitted for publication.Wang, N.; Qi, F.; Yu, H.; Yestrepsky, B.D.; Larsen, S.D.; Shi, H.; Anderson, D.W.; Li, H.; Sun, H. “Physicochemical properties and formulation development of a novel compound inhibiting Staphylococcus aureus biofilm formation”, PLOS ONE, submitted for publication.PRESENTATIONS Larsen, S. D., "A Stereoselective Synthesis of Functionalized Cyclopentenes via Base-Induced Ring Contraction of Thiocarbonyl Diels-Alder Adducts", Gordon Conference on Chemistry of Heterocyclic Compounds, New Hampton, NH, July 11-15, 1988. Larsen, S. D., Martinborough, E., "Cycloaddition of Beta-Substituted Enones to a Bicyclic Sydnone: Observation of an Unexpectedly Facile Hydrocarbon Elimination", Gordon Conference on Chemistry of Heterocyclic Compounds, New Hampton, NH, July 10-14, 1989. Larsen, S. D., Spilman, C. H., Bell, F. P., Dinh, D. M., Martinborough, E., Wilson, G. J., "Synthesis and Hypocholesterolemic Activity of 6,7-Dihydro-4H-pyrazolo[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-diones, Novel Inhibitors of AcylCoA:Cholesterol O-Acyltransferase", 201st National Meeting of the American Chemical Society, Division of Medicinal Chemistry, Atlanta, GA, April 14-19, 1991. Larsen, S.D., Spilman, C.H., Dinh, D.M., Hart, K.L., Hess, G.F., Yagi, Y., "Synthesis of a Seco-Oxysterol Inhibitor of HMG-CoA Reductase Gene Transcription", 206th National American Chemical Society Meeting, Division of Medicinal Chemistry, Chicago, IL, August 22-27, 1993. Larsen, S.D., Spilman, C.H., Dinh, D.M., Hart, K.L., Hess, G.F., Yagi, Y., "Synthesis of a Seco-Oxysterol Inhibitor of HMG-CoA Reductase Gene Transcription", 24th National Medicinal Chemistry Symposium, Salt Lake City, UT, June 21-25, 1994 . Larsen, S.D., Fisher, P.V., Libby, B.E., Mizsak, S.A., Watt, W., "Cyclopentene Synthesis via Base-Catalyzed Ring Contraction of 3,6-Dihydro-2H-thiopyrans: Studies on Diastereoselection and Mechanism", 208th National American Chemical Society Meeting, Division of Organic Chemistry, Washington, D.C., August 21-26, 1994. Watt, W., Fisher, P.V., Larsen, S.D., "A Comparison of Area Detector X-ray Diffraction Data with Conventional Diffractometer Data for Some Functionalized Cyclopentenes", 1995 Montreal American Crystallographic Association Meeting, Montreal, Quebec, Canada, July 23-28, 1995. Stevens, F.C.; Larsen, S.D., Martinborough, E.A., Burr, J.E., Connell, M.A., Shattuck, M.H., “Novel Phenylglycine-based Insulin Sensitizers: An Investigation of the Role of the alpha-Amino Acid Moiety in Antihyperglycemic Activity”, 214th National ACS Meeting, Division of Medicinal Chemistry, Las Vegas, NV, September 7-11, 1997. May, P.D.; Larsen, S.D. “Concise Synthesis of Novel 6-Substituted 2-Pyrones via Palladium-Catalyzed Cross-Coupling Methodology”, 214th National ACS Meeting, Division of Organic Chemistry, Las Vegas, NV, September 7-11, 1997. Cudahy, M.M.; Connell, M.A., Larsen, S.D.; May, P.D.; Meglasson, M.D.; Tanis, S.P.; Tegley, C.M.; Tucker, J.A.; Vaillancourt, V. “Aminoguanidines and Related Compounds as Antidiabetic Agents”, 215th National ACS Meeting, Division of Medicinal Chemistry, Dallas, TX, March 29 - April 2, 1998.Stevens, F.C.; Larsen, S.D.; Connell, M.A.; Cudahy, M.M.; Evans, B.R.; May, P.D.; Meglasson, M.D.; Tanis, S.P.; Vaillancourt, V.A. “Development of Amino- and Diaminoguanidine Antidiabetic Agents”, 215th National ACS Meeting, Division of Medicinal Chemistry, Dallas, TX, March 29 - April 2, 1998.Larsen, S.D.; Connell, M.A.; Cudahy, M.M.; Evans, B.R.; May, P.D.; Meglasson, M.D.; Stevens, F.C.; Tegley, C.M.; Tanis, S.P.; Vaillancourt, V.A. “Development of Amino- and Diaminoguanidine Antidiabetic Agents”, French American Chemical Society Meeting (FACS VII), Cannes, France, June 2-6, 1998.Larsen, S.D.; Bannow, C.A; Barf; Colca, J.R.; Herbert, N.; Laborde, A.L.; Liljebris, C.; Lindberg, T.J.; May, P.D.; Nilsson, M.C.; Ogg, D.; O'Sullivan, T.J.; Palazuk, B.J.; Rutherford-Root, K.L.; Schostarez, H.J.; Smith, C.W.; Stevens, F.C.; Stuchley, C.J.; Bleasdale, J.E. "Synthesis, Biological Activity and Enzyme-Ligand Co-crystallography of Small Molecular Weight Competitive Inhibitors of Protein Tyrosine Phosphatase 1B", invited lecture at Symposium on New Advances in Protein Tyrosine Phosphatase Inhibitors, 219th National ACS Meeting, San Francisco, California, March 26, 2000.Larsen, S.D.; Bannow, C.A; Barf; Colca, J.R.; Herbert, N.; Laborde, A.L.; Liljebris, C.; Lindberge, T.J.; May, P.D.; Nilsson, M.C.; Ogg, D.; O'Sullivan, T.J.; Palazuk, B.J.; Rutherford-Root, K.L.; Schostarez, H.J.; Smith, C.W.; Stevens, F.C.; Stuchly, C.W.; Bleasdale, J.E. "Synthesis, Biological Activity and Enzyme-Ligand Co-crystallography of Small Molecular Weight Competitive Inhibitors of Protein Tyrosine Phosphatase 1B", invited lecture at Montana State University, Bozeman, Montana, September 22, 2000.Bleasdale, J.E.; Larsen, S.D. "Protein Tyrosine Phosphatases as Drug Targets: PTP1B and Diabetes", invited lecture at Symposium on Signal Transduction, 33rd Central/Great Lakes Midwest Joint Regional ACS Meeting, Grand Rapids, Michigan, June 11-13, 2001.Larsen, S.D. “Drug Discovery from an Academic Perspective: The UM Medicinal Chemistry Core Synthesis Lab”, invited lecture at University of Michigan for INTMED/Pharm602 class: Drug Development and Clinical Trials, January 24, 2008.Fribley, A.M.; Larsen, M.J.; Cai, P.; Nerula, N.; Showalter, H.D.; Neubig, R.R.; Larsen, S.D.; Kaufman, R.J. “Complementary Cell-Based Screens Identify Specific Inhibitors of the Unfolded Protein Response Apoptotic Sub-Pathway and Reduce False Positive Hits”, Society for Biomolecular Sciences 14th Annual Meeting, St. Louis, Missouri, April 6-10, 2008.Evelyn, C.R.; Ryu, J.G.; Larsen, S.D.; Showalter, H.D.; Neubig, R.R. “Structure Activity Relationship Study of CCG-1423, an Inhibitor of Rho/MKL1-stimulated Gene Transcription”, American Association for Cancer Research Annual Meeting, San Diego, California, April 12-16, 2008.Pfefferkorn, J.A.; Choi, C.; Larsen, S.D. et al. “Pyrazoles as Hepatoselective HMG-CoA Reductase Inhibitors: Discovery and Early Clinical Evaluation of PF-3052334 for the Treatment of Hypercholesterolemia”, National Medicinal Chemistry Symposium, Abstract NMCS-124, Pittsburgh, PA, June, 2008.Okawada, M.; Koga, H.; Larsen, S.D.; Showalter, H.D.; Turbiak, A.J.; Jin, X.; Lucas, P.C.; Teitelbaum, D.H. “Use of Enterally-delivered Angiotensin II Type Ia Receptor Antagonists to Reduce the Severity of Colitis”, Annual Moses Gunn Surgery Conference, University of Michigan, Ann Arbor, MI, 2009.Okawada, M.; Koga, H.; Larsen, S.D.; Showalter, H.D.; Turbiak, A.J.; Jin, X.; Lucas, P.C.; Teitelbaum, D.H. “Use of Enterally-delivered Angiotensin II Type Ia Receptor Antagonists to Reduce the Severity of Colitis”, Digestive Disease Week of American Gastroenterology Association Annual Conference, Chicago, IL, 2009.Larsen, S.D. “Medicinal Chemistry and Drug Discovery”, invited lecture at University of Michigan for Ch/E Pharm 519 class: Modern Pharmaceutical Engineering, February 10, 2009.Larsen, S.D. “Medicinal Chemistry and Pharmaceutical Industry Research”, invited lecture at University of Michigan for Translational Strategies for ChE/BME/Pharm 596 class: Quality and Efficiency in Pharmaceutical Innovation, September 15, 2009.Larsen, S.D. “From Product Optimization to Target Identification: An Incredible Journey from Industry to Academics”; invited lecture at Paul A. Grieco 65th Birthday Symposium; Montana State University, Bozeman, MT; September 26, 2009.Larsen, S.D. “Design and Development of Highly Hepatoselective Inhibitors of HMG-CoA Reductase”, Medicinal Chemistry Department Seminar Series, University of Michigan, April 1, 2010.Xu, Y.; Ma, Y.; Larsen, S.D.; Ginsburg, D.; Sun, H. “Small Chemical Compound Inhibits Staphylococcus aureus Virulence and Accelerates HNP-1-Mediated Cell Death”, ATVB 2010, San Francisco, CA, April 8-10, 2010.Larsen, S.D. “Drug Candidate Discovery”; invited lecture at University of Michigan for PIBS 507 class: Introduction to Translational Research, January 18, 2011.Larsen, S.D. “Medicinal Chemistry and Drug Discovery”, invited lecture at University of Michigan for Ch/E Pharm 519 class: Modern Pharmaceutical Engineering, February 8, 2011.Bell, J.L.; Evelyn, C.R.; Ryu, J.G.; Wade, S.M.; Neubig, R.R.; Larsen, S.D. “Searching for the macromolecular target(s) of novel modulators of Rho signaling that inhibit prostate cancer metastasis”, 241st National ACS Meeting, Anaheim, CA, March 27-31, 2011 (MEDI-107).Larsen, S.D. “The University of Michigan Vahlteich Medicinal Chemistry Core: Leading Basic Biomedical Research down the Path of Drug Discovery”, invited lecture at Wayne State University, Detroit, MI, April 6, 2011.Yestrepsky, B.; Kretz, C.; Xu, Y.; Ginsburg, D.; Sun, H.; Larsen, S. “Virulence-attenuating inhibitors of streptokinase (SK) expression in Group A streptococcus (GAS): Activity optimization and target identification”, 242nd ACS National Meeting, Denver, CO, August 28 – September 1, 2011 (MEDI-91).Kong, W.; Burkart, A.; Chen, M.; Jin, W.; Hirshmann, M.; Goodyear, L.; Neubig, R.; Larsen, S.; Allen, P. Teg Pipes, C.G.; Bassel-Duby, R.; Olson, E.; Patti, M.-E. “Genetic or Pharmacologic Inhibition of the STARS-SRF Pathway Increases AMPK Phosphorylation and Oxidative Metabolism”, 72nd American Diabetes Assoc. Scientific Sessions, Philadelphia, PA, June 8-12, 2012.Larsen, S.D. “Novel Inhibitors of Neurotropic Alphavirus Replication That Improve Host Survival in a Mouse Model of Acute Viral Encephalitis”, invited lecture at Loyola University, Chicago, IL, March 22, 2012.Sindac, J.A.; Barraza, S.; Bolduc, K.; Yestrepsky, B.; Irani, D.; Miller, D.; Larsen, S. “Small molecule antivirals against western equine encephalitis virus”, 243rd ACS National Meeting, San Diego, CA, March 25-29, 2012 (MEDI-170).Barraza, S.J.; Sindac, J.A.; Bolduc, K.; Yestrepsky, B.; Keep, R.F.; Miller, D.J.; Larsen, S.D. “Development of novel small molecule inhibitors of alphavirus replication”, 243rd ACS National Meeting, San Diego, CA, March 25-29, 2012 (MEDI-168).Yestrepsky, B.D.; Kretz, C.; Xu, Y.; Ma, Y.; Holmes, A.; Sun, H.; Ginsburg, D.; Larsen, S.D. “SAR development and target identification studies on a class of novel bacterial virulence inhibitors”, 244th ACS National Meeting, Philadelphia, PA, August 19-23, 2012 (MEDI-260).Bolduc, K.L., Larsen, S.D., Sherman, D.H. “Chemoenzymatic synthesis of novel cryptophycin anticancer agents”, 244th ACS National Meeting, Philadelphia, PA, August 19-23, 2012 (MEDI-57).Larsen, S.D. “Development of Novel Inhibitors of Neurotropic Alphaviruses”, invited lecture at UM CDNM Lecture Series, Palmer Commons, University of Michigan, September 7, 2012.Larsen, S.D. “Novel Inhibitors of Neurotropic Alphavirus RNA Replication”, invited lecture at NERCE Medicinal Chemistry and Preclinical Development Workshop, MIT Broad Institute, Cambridge, MA, September 21, 2012.Larsen, S.D. “Medicinal Chemistry in Drug Discovery”, invited lecture at Symposium on Therapeutics Discovery & Development: Navigating the Critical Path”, Institute for Clinical and Translational Research, University of Wisconsin, Madison, WI, February 10, 2014.Barraza, S.J.; Sindac, J.A.; Dobry, C.J.; Xiang, J.; Blakely, P.K.; Irani, D.N.; Keep, R.F.; Miller, D.J.; Larsen, S.D. “Development of novel small molecule antivirals for Western equine encephalitis virus”, 247th ACS National Meeting, Dallas, TX, March 16-20, 2014 (MEDI-347).Sindac, J.A.; Barraza, Scott J.; Dobry, C.J.; Xiang, J.; Blakely, P.K.; Irani, D.N.; Keep, R.F.; Miller, D.J.; Larsen, S.D.. “Development of small molecule inhibitors against neurotropic alphavirus replication”, 247th ACS National Meeting, Dallas, TX, March 16-20, 2014 (MEDI-345).Haak, A.; Tsou, P.-S.; Fox, D.A.; Khanna, D.; Larsen, S.D.; Neubig, R.R. “Modulating myofibroblast transition in systemic sclerosis through inhibition of Rho/MRTF regulated transcription”, ASPET Annual Meeting at Experimental Biology 2014, San Diego, CA, April 26-30, 2014.Waldschmidt, H.; Homan, K.; Larimore, K.; Tesmer, J.; Larsen, S. “Development of selective GRK2 inhibitors for the treatment of heart failure”, 248th ACS National Meeting, San Francisco, CA, August 10-14, 2014 (MEDI-47).Larsen, S.D. “From Hit to Probe: Achieving In Vivo Activity with Medicinal Chemistry”, invited lecture at Drug Discovery & Development Bootcamp, University of Michigan, Ann Arbor, MI, March 16, 2015.Larsen, S.D. "The University of Michigan Vahlteich Medicinal Chemistry Core: Achieving Proof-of-Concept in Vivo for Novel Therapeutic Hypotheses”, invited lecture at 2015 Great Lakes/Central Regional ACS Meeting, May 27-29, 2015 (JGLCRM 31).Carruthers, V.B; Zwicker, J.; Haug, N.; Banda, A.; Diaz, N; Schultz, T.L.; DiCristina, M.; Larsen, S.D. “Targeting a T. gondii cathepsin protease essential for chronic toxoplasmosis” Keystone Symposia on Molecular and Cellular Biology, Drug Discovery for Parasitic Diseases, Tahoe City, CA, January 24-28, 2016.Waldschmidt, H.V.; Homan, K.T.; Cruz-Rodriguez, O.; Cato, M.; Larimore, K.; Cannavo, A.; Song, J.; Cheung, J.Y.; Koch, W.J.; Tesmer, J.J.G.; Larsen, S.D., “Development of Selective GRK2 inhibitors for the Treatment of Heart Failure”, Keystone Symposia on Molecular and Cellular Biology, G Protein-Coupled Receptors: Structure, Signaling and Drug Discovery, February 21-25, 2016.Larsen, S.D. "The University of Michigan Vahlteich Medicinal Chemistry Core: Achieving Proof-of-Concept in Vivo for Academic Drug Discovery”, invited lecture, Michigan State University Department of Pharmacology & Toxicology Seminar Series, March 11, 2016.Diaz, N.; Zwicker, J.; Larsen, S.; Carruthers, V. “Design and synthesis of potential CNS-?permeable inhibitors of T. gondii Cathepsin L”, 251st ACS National Meeting, San Diego, CA, March 13-17, 2016 (MEDI-99).Larsen, S.D., “Development of CNS-Permeable Glucosylceramide Synthase Inhibitors for the Treatment of Neuronopathic Lipid Storage Diseases”, invited lecture, 2017 Endolysosomal Function in Health & Disease Symposium, Ann Arbor, MI, April 14, 2017.Waldschmidt, H.; Homan, K.; Cruz-Rodriguez, O.; Cato, M.; Bouley, R.; Wilson, M.; Cannavo, A.; Song, J.; Cheung, J.; Kirchhoff, P.; Koch, W.; Tesmer, J.; Larsen, S.D. “Metamorphosis of paroxetine into a highly potent and selective GRK2 inhibitor via structure-?based drug design”, 253rd ACS National Meeting, San Francisco, CA, April 2-6, 2017 (MEDI-10).Huddle, Brandt; Yang, K.; Chtcherbinine, M.; Chefetz-Menaker, I.; Morgan, C.; Buckanovich, R.; Hurley, T.; Larsen, S. “Development of cancer stem cell depleting ALDH1A selective inhibitors as potential therapeutics for ovarian cancer”, 253rd ACS National Meeting, San Francisco, CA, April 2-6, 2017 (MEDI-221).Larsen, S.D.; Shayman, J.A. “Development of CNS-Permeable Inhibitors of Glucosylceramide Synthase for Neuronopathic Lipid Storage Diseases”, invited lecture, 48th Central Regional ACS Meeting, Dearborn, MI, June 7, 2017 (CERM-2).Neubig RR, Lisabeth EM, Hutchings K, Dexheimer T, Khanna D, Fox DA, Larsen SD “Optimization of gene transcription inhibitors as novel oral anti-fibrotic agents”, 15th International Workshop on Scleroderma Research, Pittsburgh, PA, August 5-9, 2017.Lisabeth EM, Kahl D, Gopallawa I, Haynes SE, Misek SA, Khanna D, Fox DA, Martin BR, Larsen SD, Neubig RR “Identification of Pirin as a novel therapeutic target of CCG-222740 in fibrosis”, 15th International Workshop on Scleroderma Research, Pittsburgh, PA, August 5-9, 2017Zwicker, J.; Haug, N.; Diaz, N.; Christina, M.; Carruthers, V.; Larsen, S.D. “Design and synthesis of selective and brain penetrant inhibitors of Toxoplasma Gondii cathepsin L”, 72nd Northwest Regional ACS Meeting, Corvalis, OR, June 25-28, 2017 (NORM-24).Kahl, D.; Lisabeth, M.; Haynes, S.; Martin, B.; Neubig, R.; Larsen, S. “Development of affinity probes for identification of the molecular target for a novel series of Rho?/MRTF?/SRF-?mediated gene transcription inhibitors”, 254th National ACS Meeting, Washington, DC, August 20-24, 2017 (MEDI-6161).Zwicker, J.D.; Smith, D.; Guerra, A.J.; Hitchens, J.; Kirchhoff, P.D.; Wen, B.; Sun, D.; White, A.D.; Larsen, S.D.; Carruthers, V.B. “Triazine nitriles targeting Cathepsin Protease L and chronic Toxoplasma infection”, 15th International Toxoplasma Congress, June 19-22, 2019,?Quindio, Colombia.PATENTS AND PUBLISHED APPLICATIONS (PHARMA)US 5,132,424: Pyrazolo-pyrrolo-pyrimdine-diones.US 5,523,318: Pyrrolidino-substituted oximes useful as anti-atherosclerosis and anti-hypercholesterolemic agents.US 5,565,468: Pyridino substituted oximes useful as anti-atherosclerosis and anti-hypercholesterolemic agents.US 5,597,816: Pyrazoloazepino substituted oximes useful as anti-atherosclerosis and anti-hypercholesterolemic agents.US 5,723,476: 4-Hydroxycoumarin-3-carboxamides for the treatment of diabetes mellitus.US 5,955,617: Aminoguanidine carboxylate lactams for the treatment of non-insulin-dependent diabetes mellitus.US 5,994,577: Aminoguanidine carboxylates for the treatment of non-insulin-dependent diabetes mellitus.US 6,166,080: Aminoguanidine carboxylates for the treatment of obesity.US 6,177,453: Aminoguanidine carboxylate lactams for the treatment of non-insulin-dependent diabetes mellitus.US 6,184,216: Aminoguanidine carboxylate lactams for the treatment of non-insulin-dependent diabetes mellitus.US 6,624,160: 4-oxo-1,4-dihydro-3-cinnolinecarboxamides as antiviral agentsUS 6,274,580: Aminoguanidine carboxylate lactams for the treatment of non-insulin-dependent diabetes mellitus.US 6,329,545: Aminoguanidine carboxylates for the treatment of non-insulin-dependent diabetes mellitus.US 6,353,023: Inhibitors of protein tyrosine phosphatases.US 6,410,585: Inhibitors of protein tyrosine phosphatases.US 6,458,788: 4-Hydroxycinnoline-3-carboxyamides as antiviral agentsUS 6,624,160: 4-Oxo-1,4-dihydro-3-cinnolinecarboxamides as antiviral agentsUS 6,852,731: Antiviral compoundsUS 6,861,438: Antiviral agentsUS 8,895,748: Synthesis for thiazolidinedione compoundsUS 8,912,335: PPAR-sparing thiazolidinedione salts for the treatment of metabolic diseasesUS 8,937,182: Synthesis for thiazolidinedione compoundsUS 8,946,435: Synthesis for thiazolidinedione compoundsUS 9,126,959: PPAR-sparing thiazolidinedione salts for the treatment of metabolic diseasesUS 9,562,012: PPAR-sparing compounds for the treatment of metabolic diseasesWO200204444: Heterocycle carboxamides as antiviral agents.WO200204443: Heterocycle carboxamides as antiviral agents.WO2003059912: Preparation of 7-oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides as antiviral compounds.WO2003059878: Preparation of 7-oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides as antiviral compounds. US2004138449: A preparation of thieno[2,3-b]pyridinecarboxamide derivatives, useful as antiviral agentsWO2005079790: Preparation of imidazole-based HMG-CoA reductase inhibitorsWO2006087630: Preparation of pyrazolyloxy hexanoic acid derivatives as HMG CoA reductase inhibitorsWO2008104875: Oxazolidinones as cholesterol absorption inhibitorsWO2010105048: Preparation of benzylthiazolidinedione derivatives for use as PPAR? modulatorsWO2011075514: PPAR-sparing thiazolidinediones and combinations for the treatment of neurodegenerative diseases.WO2011084453: PPAR-sparing thiazolidinedione salts for the treatment of metabolic diseasesWO2011084456: PPAR-sparing thiazolidinediones and combinations for the treatment of diabetes mellitus and other metabolic diseasesWO2011084459: PPAR-sparing thiazolidinediones and combinations for the treatment of obesity and other metabolic diseasesWO2011133442: Novel synthesis for thiazolidinedione compoundsWO2012021467: A process for the preparation of thiazolidinedione derivatives for use as PPAR? receptor modulatorsWO2012178142: Prepration of indolylmethylphenoxypropranoic acid derivatives and analogs for use as PPAR modulators.WO 2012177956: Preparation of phenyloxoethylphenylacrylate derivatives and analogs for use as PPAR modulatorsWO2015013187: Preparation of phenylalkylhydroxamate derivatives for use in the treatment of metabolic diseasesPATENTS AND PUBLISHED APPLICATIONS (UNIVERSITY OF MICHIGAN)US 8,293,776: Compositions and methods for treating inflammatory conditions of the bowel.US 8,501,722: Methods and compositions for treating bacterial infectionUS 8,846,684: Arbovirus inhibitors and uses thereof.US 8,865,750: Small molecule inhibitors of RGS proteins US 8,946,424: Deuterated amlexanoxUS 8,961,959: Glucosylceramide Synthase Inhibitors and Therapeutic Methods Using the SameUS 9,365,581: Deuterated amlexanoxUS 9,468,632: Methods and compositions for targeting cancer stem cellsUS 9,504,688: Methods and compositions for treating bacterial infectionUS 9,598,441: Therapeutic compounds and methodsUS 9,944,652: Deuterated amlexanoxUS 10,023,564: G protein-coupled receptor kinase 2 inhibitors and methods for use of the sameUS 10,202,340: Glucosylceramide synthase inhibitors and therapeutic methods using the sameUS 10,329,283: G protein-coupled receptor kinase inhibitors and methods for use of the sameUS 10,662,183 Inhibitors of myocardin-related transcription factor and serum response factor (MRTF/SRF)-mediated gene transcription and methods for use of the same.WO2011035143: Benzamides and related compounds as RhoGTPase inhibitors and their preparation and compositions for inhibiting Rho-mediated diseases and conditions.WO2012149335: Preparation of thiadiazolidinone derivatives as inhibitors of RGS proteinsWO 2013033392: Antitumor compounds.WO2013166282: Preparation of benzoquinazoline derivatives for treating bacterial infection.WO2014085485: Methods and compositions for targeting cancer stem cells.WO 2014179734: Preparation of deuterated amlexanox derivatives for use as TBK1 or IKKε protein kinase inhibitorsUS20150250769: Methods and compositions for inhibiting Rho/MRTF-mediated diseases and conditionsWO2016023028: G protein-coupled receptor kinase 2 inhibitors and methods for use of the sameWO2016073847: Preparation of substituted piperidine-3-carboxamides as inhibitors of myocardin-?related transcription factor and serum response factor (MRTF/SRF)?-?mediated gene transcriptionWO2016126572: Preparation of indanylacetamide derivatives as glucosylceramide synthase inhibitors and therapeutic methods thereofWO2016210403: Preparation of substituted piperidines as G protein-?coupled receptor kinase inhibitors and methods for use of the sameWO2017223086: Preparation of thiopyrimidinone-?based small molecule inhibitors of aldehyde dehydrogenase (ALDH) for targeting cancer stem cellsWO2019195641: Preparation of aryloxadiazoles as inhibitors of Rho?/MRTF?/SRF-?mediated gene transcription and methods for use of the same ................
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