CURRICULUM VITAE
John McCorvy PhD
John McCorvy PhD
Associate Professor
Department of Cell Biology, Neurobiology and Anatomy
Department of Cell Biology, Neurobiology and Anatomy
OFFICE ADDRESS: |
Basic Science Building |
8701 Watertown Plank Rd |
Milwaukee, WI 53226 |
Email: jmccorvy@mcw.edu |
EDUCATION: |
2000 - 2005 B.A. Biochemistry and Psychology, magna cum laude, Texas Tech University, Lubbock, TX |
2006 - 2012 Ph.D., Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN |
POSTGRADUATE TRAINING AND FELLOWSHIP APPOINTMENTS: |
2012 - 2018 Post Doctoral Researcher/Research Associate, Department of Pharmacology, Division of Chemical Biology and Medicinal Chemistry, University of North Carolina Chapel Hill Medical School, Chapel Hill, NC |
FACULTY APPOINTMENTS: |
2018 - Present Assistant Professor, Cell Biology, Neurobiology, and Anatomy, Medical College of Wisconsin, Milwaukee, WI |
2023 - Present NIH study section, Drug Discovery and Molecular Pharmacology B, ad hoc member |
2023 - Present NIDA study section, Avenir Award Program for Chemistry and Pharmacology of Substance Use Disorders |
AWARDS AND HONORS: |
2000 - 2002 McFaddens-Leaders Scholarship, Texas Tech University |
2006 - 2007 Lynn Fellowship , Purdue University |
2008 Best Presentation, Purdue University Neuroscience |
2010 Kienly Award for Excellence in Teaching , Purdue University |
2012 Bilsland Fellowship , Purdue University |
2012 1st Place Poster Prize , Sigma Xi Poster Presentation |
2015 Best Poster Prize , Great Lakes GPCR Retreat |
2016 Postdoctoral Scholar Award , UNC Pharmacology Department |
2018 Trainee Travel Award, International Society for Serotonin Research |
2019 Neuroscience Research Center Excellence Award, Medical College of Wisconsin |
2020 - 2022 Outstanding Graduate School Educator, Medical College of Wisconsin |
MEMBERSHIPS IN HONORARY AND PROFESSIONAL SOCIETIES: |
2013 - Present International Society for Serotonin Research (Member) |
2016 - Present Society for Neuroscience (Member) |
2019 - Present International Society for Research Psychedelics (Member) |
2019 - Present American Chemical Society (Member) |
EDITORSHIPS/EDITORIAL BOARDS/JOURNAL REVIEWS: |
Ad-Hoc Reviewer |
2016 Journal of Receptor Signal Transduction |
2016 - 2022 Nature Communications |
2016 British Journal of Pharmacology |
2017 PLoS Computational Biology |
2017 Molecular Psychiatry |
2018 - 2022 Nature |
2018 - 2023 ACS Chemical Biology |
2018 Nature Structural and Molecular Biology |
2018 - 2023 ACS Chemical Neuroscience |
2019 - 2022 Neuropharmacology |
2019 Journal of Pharmacology and Experimental Therapeutics |
2020 European Neuropharmacology |
2020 - 2022 Scientific Reports |
2021 Journal of Neurochemistry |
2021 Journal of Medicinal Chemistry |
2021 - 2023 ACS Pharmacology and Translational Science |
2021 Journal of Molecular Structure |
2021 Journal of Biological Chemistry |
2021 Frontiers in Pharmacology |
2022 Structure |
2022 Experimental Neurology |
2022 - 2023 Nature Chemical Biology |
2023 Psychedelic Medicine |
2023 Biochemistry ACS |
LOCAL/REGIONAL APPOINTED LEADERSHIP AND COMMITTEE POSITIONS: |
2019 - 2023 Member, Former Chair, IDP Website Design Committee, Medical College of Wisconsin |
2020 Member, Research Culture Workgroup Committee, Medical College of Wisconsin |
2020 Member, Department of Pharmacology Chair Search, Medical College of Wisconsin |
2021 - Present Member, Cancer Center Structural Biology Faculty Search Committee, Medical College of Wisconsin |
2021 - 2022 Member, Program in Chemical Biology Faculty Search Committee, Medical College of Wisconsin |
RESEARCH GRANTS/AWARDS/CONTRACTS/PROJECTS: | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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INVITED LECTURES/WORKSHOPS/PRESENTATIONS: |
International |
Molecular recognition of serotonin receptors, International Society for Serotonin Research, Arabella, South Africa, 2014 |
Atomic-level resolution of serotonin receptor signaling, International Society for Serotonin Research, Seattle, WA, 2016 |
Time-dependent biased signaling of the 5-HT2A receptor, International Society for Serotonin Research, Cork, Ireland, 2018 |
Structural determinants of serotonin receptor recognition and activation, International Society for Serotonin Research, Cork, Ireland, 2018 |
Psychedelic Superagonism and Functional Selectivity Profiling at the Serotonin Receptors, International Society for Research into Psychedelics, New Orleans, LA, 2019 |
Surveying the 5-HT2C-selective agonist landscape: What’s selective and what’s not?
Part of symposia on 5-HT2C Mechanisms and Drug Discovery-organizer, International Society for Serotonin Research, Cancun, Mexico, 2023 |
Development of Assay Platforms for Polypharmacological Drug Discovery, Otsuka Pharmaceuticals, Tokoyo, Japan, 2023 |
National |
Structure-guided discovery of biased dopamine and serotonin ligands: Lessons from the LSD crystal structure, University of Minnesota Twin Cities Department of Pharmacology, Minneapolis, MN, 2016 |
Structure-based and Rational Design of Biased GPCR Ligands with Improved Therapeutic Profiles, Discovery on Target Drug Symposia, Virtual, 2022 |
Beyond Psychedelics: Venturing into a New Era of Serotoninergic Drug Discovery, 2nd Annual Psychedelic Therapeutics & Drug Conference, Washington, DC, 2022 |
Panel Discussion: Psychedelics: Has Nature Given Us All We Need?, SXSW, Austin, Texas, 2022 |
Panel Discussion: Biased Signaling: From Pharmacology to Physiology, Discovery on Target Drug Symposia, Virtual, 2022 |
Regional |
Profiling Psychedelics for Antidepressant Effects, Usona Institute, Madison, WI, 2018 |
Toward a molecular understanding of GPCR drug action, Promega Corporation, Madison, WI, 2018 |
Profiling Psychedelics at the Serotonin Receptors, BTCI Consciousness Forum, Madison, WI, 2019 |
Psychedelic Therapeutics and Transforming the Future of Mental Health Care, BioForward Wisconsin Health Summit, Virtual, 2021 |
Next-generation Psychedelics: A Focus on Molecular Mechanisms of Serotonin GPCRs, Promega Corporation, Madison, WI, 2023 |
Local |
Doxanthrine, a novel D1 agonist, attenuates DOI-induced ear scratch in mice, Purdue Neuroscience Retreat, West Lafayette, IN, 2007 |
Dopamine D1 selective drugs: Evaluation using locomotor activity and the 6-hydroxydopamine lesion model, Purdue Neuroscience Retreat, West Lafayette, IN, 2008 |
Fine-tuning GPCRs toward biased signaling: Implications for novel therapeutic strategies, Medical College of Wisconsin, Milwaukee, WI, 2017 |
Uncovering Biased Signaling at GPCRs for Novel Drug Design Approaches, Medical College of Wisconsin Biochemistry Department, Milwaukee, WI, 2019 |
Uncovering Biased Signaling at GPCRs for Novel Drug Design Approaches, Medical College of Wisconsin Department of Physiology, Milwaukee, WI, 2019 |
Structure-based Approaches Toward Pathway-Selective GPCR Drug Discovery, Medical College of Wisconsin Cancer Center, Milwaukee, WI, 2020 |
Psychedelic Drug Discovery in a New Era, Medical College of Wisconsin Pharmacology Department, Milwaukee, WI, 2023 |
Search for New Rapid-Acting Mental Health Treatments, Froedert Hospital Administration, Milwaukee, WI, 2023 |
PEER REVIEWED WORKSHOPS/PRESENTATIONS: |
International |
Retention of drug stimulus control in pigeons trained to a three-key morphine discrimination, College of Problems of Drug Dependence, Quebec, Canada, 2007 |
LSD bound crystal structure reveals atomic basis of serotonin receptor signaling, International Society for Serotonin Research, Seattle, WA, 2016 |
Time-dependent biased signaling at the 5-HT2A receptor, International Society for Serotonin Research, Cork, Ireland, 2018 |
National |
Efficacy of functionally selective dopamine D2 Receptor ligands on schizophrenia-like behaviors, American College of Neuropsychopharmacology, Phoenix, AZ, 2014 |
Regional |
Uncovering the molecular basis of B-arrestin bias at the dopamine D2 receptor, Great Lake GPCR Retreat, Quebec, Canada, 2014 |
Discovery of novel dopamine D2 G protein-biased ligands, Great Lakes GPCR Retreat, Toronto, Canada, 2015 |
Orthosteric and allosteric activation mechanisms of the 5-HT2B receptor, Great Lakes GPCR Retreat, Chicago, IL, 2016 |
Local |
Molecular interactions of psychedelics with the serotonin 5-HT2A receptor, Sigma Xi Poster Competition, West Lafayette, IN, 2012 |
COMMITTEE SERVICE: |
Medical College of Wisconsin |
2019 - 2023 Chair, IDP Website Committee |
2020 Member, Research Culture Workgroup Member |
2020 Member, Department of Pharmacology Chair Search |
2021 - 2022 Member, Program in Chemical Biology Faculty Search |
2021 - 2023 Member, Cancer Center Structural Biology Faculty Search |
MCW TEACHING ACTIVITIES: |
Medical Student Education |
2024 - Present Lecturer, Neuroscience, Anitmigraine and Serotonin Drugs |
Graduate Student Education |
2019 - Present Lecturer, Understanding Cell Signaling Through Therapeutic Drugs |
2019 - Present Lecturer, Fundamentals of Neuroscience |
EXTRAMURAL TEACHING: |
Medical Student Education |
2003 - 2005 Texas Tech University, Teaching Assistant, General Chemistry |
2004 - 2005 Texas Tech University, Teaching Assistant, Organic Chemistry |
Pharmacy Student Education |
2007 - 2011 Purdue University, Head Teaching Assistant, Neuropharmacology |
2008 - 2010 Purdue University, Teaching Assistant, Renal and Cardiovascular Pharmacology |
Graduate Student Education |
2016 - 2017 University of North Carolina, Chapel Hill, Head Instructor, Cellular and Molecular Neuroscience: Biased GPCR Signaling |
MCW STUDENTS, FACULTY, RESIDENTS AND CLINICAL/RESEARCH FELLOWS MENTORED: |
Graduate Students |
Students Advised |
2019 Jacob Adelman, Rotation Student, Neuroscience Doctoral Program, Medical College of Wisconsin |
2019 - 2020 Gage Stuttgen, Rotation Student, Interdisciplinary Doctoral Program (IDP), Medical College of Wisconsin |
2019 Zachary Plautz, Rotation Student, Medical Scientist Training Program (MSTP), Medical College of Wisconsin |
2019 Kyle McLaughlin, Rotation Student, Neuroscience Doctoral Program (NDP), Medical College of Wisconsin |
2023 Kaitlyn Partridge, Rotation Student, Neuroscience Doctoral Program (NDP), Medical College of Wisconsin |
2023 Mallika Khurana, Rotation Student, Interdiscplinary Doctoral Program (IDP), Medical College of Wisconsin |
PhD Committees |
2020 - 2023 Donovan Drouillard, Role of CCR6 and CCL20 signaling axis in anti-tumor T cell Responses, Medical College of Wisconsin |
2020 - 2023 Courtney Fisher, Mechanistic Insights into Novel A3 Adenosine Receptor Allosteric Modulators, Medical College of Wisconsin |
2021 - Present Dianise Rodriguez, Mechanisms Underlying CGRP-induced Migraine, Medical College of Wisconsin |
2021 - Present Roman Schlimgen, Structural Basis of Nanobody-induced Chemokine Receptor Inhibition, Medical College of Wisconsin |
2022 - Present Claudia Rohr, Functional interrogation of parasitic flatworm TRPM channels to identify
novel antihelmintics, Medical College of Wisconsin |
2023 - Present Alex Garces, Development of EPR autosampling technologies for interrogation of GPCR
Conformations, Medical College of Wisconsin |
PhD |
2020 - Present Nicholas Malcolm, Medical Scientist Training (MSTP) student, Medical College of Wisconsin, National presentations, peer-review publications, mentoring plan |
2021 - Present Emma Bonniwell, Neuroscience Doctoral (NDP) Student, Medical College of Wisconsin, National presentations, peer-review publications, mentoring plan |
2021 - Present Janelle Lanham, Interdisciplinary Doctoral (IDP) Graduate Student, Medical College of Wisconsin, National presentations, peer-review publications, mentoring plan |
Postdoctoral Students |
2021 - 2022 Daniel Sprague, Postdoctoral Researcher, Medical College of Wisconsin |
2022 - Present Tyler Fenske, Postdoctoral Researcher, Medical College of Wisconsin |
Clinical Staff |
2018 - 2019 Emilie Anderson, Research Technician, Medical College of Wisconsin |
2018 - 2021 Lauren Laskowski, Research Technician, Medical College of Wisconsin |
2021 - Present Hailey Hammen, Research Technician, Medical College of Wisconsin |
2021 - 2022 Andrew Cao, Research Technician, Medical College of Wisconsin |
2021 - 2022 Maggie Calkins, Research Technician, Medical College of Wisconsin |
2021 - 2022 Alisha Shaikh, Research Technician, Medical College of Wisconsin |
2022 - 2023 Marco Ivancich, Research Technician, Medical College of Wisconsin |
2022 - 2023 Joseph Hennessey, Research Technician, Medical College of Wisconsin |
2023 - Present Allison Clark, Research Technician, Medical College of Wisconsin |
2023 - Present Natalie Cavalco, Research Technician, Medical College of Wisconsin |
2023 - Present Josie Lammers, Research Technician, Medical College of Wisconsin |
EXTRAMURAL STUDENTS, FACULTY, RESIDENTS, AND CLINICAL/RESEARCH FELLOWS MENTORED: |
Undergraduate Students |
2008 - 2010 Aubrie Harland, Undergraduate Researcher, Purdue University |
2010 - 2012 Whitney Williams, Undergraduate Researcher, Purdue University |
2012 Rachel Slater, Visiting Undergraduate Researcher, Trinity College Dublin |
2013 Katie Rechsteiner, Undergraduate Researcher, University of North Carolina |
2014 Alia Capone, Undergraduate Researcher, University of North Carolina |
2015 Bemnat Agenehu, Undergraduate Researcher, University of North Carolina |
2016 Ariana Gavin, Undergraduate Researcher, University of North Carolina |
2017 - 2018 Alexandra Tribo, Undergraduate Researcher, University of North Carolina |
MEDIA APPEARANCES: |
2022 SXSW Psychedelics: Has Nature Given Us Al We Need?
https://www.youtube.com/watch?v=ChIET4UI5N4
|
2023 - Present Bill would allow veterans to treat PTSD with psychedelic mushrooms
https://www.cbs58.com/news/bill-would-allow-veterans-to-treat-ptsd-with-psychedelic-mushrooms |
PATENTS: |
2021 3-(2-(aminoethyl)-indol-4-ol derivatives, methods of preparation thereof, and the use as 5-HT2 receptor modulators
Alan Kozikowski, Gideon Shapiro, Werner Tueckmantel, John McCorvy
In partnership with BrightMinds Bio |
2021 Heterocyclic Compounds and Methods of Preparation Thereof
Alan Kozikowski, Uros Laban, Werner Tueckmantel, John McCorvy
In partnership with BrightMinds Bio
|
2021 Selective, Partial, and Arrestin-Biased 5-HT2A Agonists with Utility in Various Disorders
Jason Wallach, John McCorvy, Adam Halberstadt
In partnership with University of the Sciences and UCSD
|
BIBLIOGRAPHY |
Refereed Journal Publications/Original Papers |
1. Przybyla JA, Cueva JP, Chemel BR, Hsu KJ, Riese DJ 2nd, McCorvy JD, Chester JA, Nichols DE, Watts VJ. Comparison of the enantiomers of (+/-)-doxanthrine, a high efficacy full dopamine D(1) receptor agonist, and a reversal of enantioselectivity at D(1) versus alpha(2C) adrenergic receptors. Eur Neuropsychopharmacol. 2009 Feb;19(2):138-46. PMCID: PMC2636714 |
2. Clark LH, Cueva JP, McCorvy JD, Harland AA, Watts VJ, Nichols DE. C-Ring expanded analogs of doxanthrine: Conformation plays a critical role Arkivoc. 29 January 2011;2010(4):125-138. |
3. McCorvy JD, Harland AA, Maglathlin R, Nichols DE. A 5-HT(2C) receptor antagonist potentiates a low dose amphetamine-induced conditioned place preference. Neurosci Lett. 2011 Nov 07;505(1):10-3. PMCID: PMC3213641 |
4. Clark AH, McCorvy JD, Watts VJ, Nichols DE. Assessment of dopamine D₁ receptor affinity and efficacy of three tetracyclic conformationally-restricted analogs of SKF38393. Bioorg Med Chem. 2011 Sep 15;19(18):5420-31. PMCID: PMC3171562 |
5. McCorvy JD, Watts VJ, Nichols DE. Comparison of the D₁ dopamine full agonists, dihydrexidine and doxanthrine, in the 6-OHDA rat model of Parkinson's disease. Psychopharmacology (Berl). 2012 Jul;222(1):81-7. |
6. Clark AH, McCorvy JD, Conley JM, Williams WK, Bekkam M, Watts VJ, Nichols DE. Identification of a 2-phenyl-substituted octahydrobenzo[f]quinoline as a dopamine D₃ receptor-selective full agonist ligand. Bioorg Med Chem. 2012 Nov 01;20(21):6366-74. PMCID: PMC3505999 |
7. Pigott A, Frescas S, McCorvy JD, Huang XP, Roth BL, Nichols DE. trans-2-(2,5-Dimethoxy-4-iodophenyl)cyclopropylamine and trans-2-(2,5-dimethoxy-4-bromophenyl)cyclopropylamine as potent agonists for the 5-HT(2) receptor family. Beilstein J Org Chem. 2012;8:1705-9. PMCID: PMC3511003 |
8. Juncosa JI Jr, Hansen M, Bonner LA, Cueva JP, Maglathlin R, McCorvy JD, Marona-Lewicka D, Lill MA, Nichols DE. Extensive rigid analogue design maps the binding conformation of potent N-benzylphenethylamine 5-HT2A serotonin receptor agonist ligands. ACS Chem Neurosci. 2013 Jan 16;4(1):96-109. PMCID: PMC3547484 |
9. Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC. Structural features for functional selectivity at serotonin receptors. Science. 2013 May 03;340(6132):615-9. PMCID: PMC3644390 |
10. Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou XE, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE. Structural basis for molecular recognition at serotonin receptors. Science. 2013 May 03;340(6132):610-4. PMCID: PMC3644373 |
11. Hansen M, Jacobsen SE, Plunkett S, Liebscher GE, McCorvy JD, Bräuner-Osborne H, Kristensen JL. Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists. Bioorg Med Chem. 2015 Jul 15;23(14):3933-7. |
12. Kroeze WK, Sassano MF, Huang XP, Lansu K, McCorvy JD, Giguère PM, Sciaky N, Roth BL. PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome. Nat Struct Mol Biol. 2015 May;22(5):362-9. PMCID: PMC4424118 |
13. Cheng J, Giguere PM, Schmerberg CM, Pogorelov VM, Rodriguiz RM, Huang XP, Zhu H, McCorvy JD, Wetsel WC, Roth BL, Kozikowski AP. Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. J Med Chem. 2016 Jan 28;59(2):578-91. PMCID: PMC8317212 |
14. Farrell MS, McCorvy JD, Huang XP, Urban DJ, White KL, Giguere PM, Doak AK, Bernstein AI, Stout KA, Park SM, Rodriguiz RM, Gray BW, Hyatt WS, Norwood AP, Webster KA, Gannon BM, Miller GW, Porter JH, Shoichet BK, Fantegrossi WE, Wetsel WC, Roth BL. In Vitro and In Vivo Characterization of the Alkaloid Nuciferine. PLoS One. 2016;11(3):e0150602. PMCID: PMC4786259 |
15. Chan JD, McCorvy JD, Acharya S, Johns ME, Day TA, Roth BL, Marchant JS. A Miniaturized Screen of a Schistosoma mansoni Serotonergic G Protein-Coupled Receptor Identifies Novel Classes of Parasite-Selective Inhibitors. PLoS Pathog. 2016 May;12(5):e1005651. PMCID: PMC4871480 |
16. Manglik A, Lin H, Aryal DK, McCorvy JD, Dengler D, Corder G, Levit A, Kling RC, Bernat V, Hübner H, Huang XP, Sassano MF, Giguère PM, Löber S, Da Duan, Scherrer G, Kobilka BK, Gmeiner P, Roth BL, Shoichet BK. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Sep 08;537(7619):185-190. PMCID: PMC5161585 |
17. Cheng J, McCorvy JD, Giguere PM, Zhu H, Kenakin T, Roth BL, Kozikowski AP. Design and Discovery of Functionally Selective Serotonin 2C (5-HT<sub>2C</sub>) Receptor Agonists. J Med Chem. 2016 Nov 10;59(21):9866-9880. |
18. Chen X, McCorvy JD, Fischer MG, Butler KV, Shen Y, Roth BL, Jin J. Discovery of G Protein-Biased D2 Dopamine Receptor Partial Agonists. J Med Chem. 2016 Dec 08;59(23):10601-10618. PMCID: PMC5148701 |
19. Urs NM, Gee SM, Pack TF, McCorvy JD, Evron T, Snyder JC, Yang X, Rodriguiz RM, Borrelli E, Wetsel WC, Jin J, Roth BL, O'Donnell P, Caron MG. Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties. Proc Natl Acad Sci U S A. 2016 Dec 13;113(50):E8178-E8186. PMCID: PMC5167191 |
20. Wacker D, Wang S, McCorvy JD, Betz RM, Venkatakrishnan AJ, Levit A, Lansu K, Schools ZL, Che T, Nichols DE, Shoichet BK, Dror RO, Roth BL. Crystal Structure of an LSD-Bound Human Serotonin Receptor. Cell. 2017 Jan 26;168(3):377-389.e12. PMCID: PMC5289311 |
21. Lansu K, Karpiak J, Liu J, Huang XP, McCorvy JD, Kroeze WK, Che T, Nagase H, Carroll FI, Jin J, Shoichet BK, Roth BL. In silico design of novel probes for the atypical opioid receptor MRGPRX2. Nat Chem Biol. 2017 May;13(5):529-536. PMCID: PMC5391270 |
22. Jensen AA, McCorvy JD, Leth-Petersen S, Bundgaard C, Liebscher G, Kenakin TP, Bräuner-Osborne H, Kehler J, Kristensen JL. Detailed Characterization of the In Vitro Pharmacological and Pharmacokinetic Properties of <i>N</i>-(2-Hydroxybenzyl)-2,5-Dimethoxy-4-Cyanophenylethylamine (25CN-NBOH), a Highly Selective and Brain-Penetrant 5-HT<sub>2A</sub> Receptor Agonist. J Pharmacol Exp Ther. 2017 Jun;361(3):441-453. |
23. Hoehn RD, Nichols DE, McCorvy JD, Neven H, Kais S. Experimental evaluation of the generalized vibrational theory of G protein-coupled receptor activation. Proc Natl Acad Sci U S A. 2017 May 30;114(22):5595-5600. PMCID: PMC5465905 |
24. Brandt SD, Kavanagh PV, Twamley B, Westphal F, Elliott SP, Wallach J, Stratford A, Klein LM, McCorvy JD, Nichols DE, Halberstadt AL. Return of the lysergamides. Part IV: Analytical and pharmacological characterization of lysergic acid morpholide (LSM-775). Drug Test Anal. 2018 Feb;10(2):310-322. PMCID: PMC6230476 |
25. Zhang G, Cheng J, McCorvy JD, Lorello PJ, Caldarone BJ, Roth BL, Kozikowski AP. Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. J Med Chem. 2017 Jul 27;60(14):6273-6288. PMCID: PMC7374938 |
26. Wang S, Wacker D, Levit A, Che T, Betz RM, McCorvy JD, Venkatakrishnan AJ, Huang XP, Dror RO, Shoichet BK, Roth BL. D<sub>4</sub> dopamine receptor high-resolution structures enable the discovery of selective agonists. Science. 2017 Oct 20;358(6361):381-386. PMCID: PMC5856174 |
27. Chan JD, Cupit PM, Gunaratne GS, McCorvy JD, Yang Y, Stoltz K, Webb TR, Dosa PI, Roth BL, Abagyan R, Cunningham C, Marchant JS. The anthelmintic praziquantel is a human serotoninergic G-protein-coupled receptor ligand. Nat Commun. 2017 Dec 05;8(1):1910. PMCID: PMC5716991 |
28. McCorvy JD, Butler KV, Kelly B, Rechsteiner K, Karpiak J, Betz RM, Kormos BL, Shoichet BK, Dror RO, Jin J, Roth BL. Structure-inspired design of β-arrestin-biased ligands for aminergic GPCRs. Nat Chem Biol. 2018 Feb;14(2):126-134. PMCID: PMC5771956 |
29. Che T, Majumdar S, Zaidi SA, Ondachi P, McCorvy JD, Wang S, Mosier PD, Uprety R, Vardy E, Krumm BE, Han GW, Lee MY, Pardon E, Steyaert J, Huang XP, Strachan RT, Tribo AR, Pasternak GW, Carroll FI, Stevens RC, Cherezov V, Katritch V, Wacker D, Roth BL. Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor. Cell. 2018 Jan 11;172(1-2):55-67.e15. PMCID: PMC5802374 |
30. Peng Y, McCorvy JD, Harpsøe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjørn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng J, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ. 5-HT<sub>2C</sub> Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology. Cell. 2018 Feb 08;172(4):719-730.e14. PMCID: PMC6309861 |
31. Qin S, Meng M, Yang D, Bai W, Lu Y, Peng Y, Song G, Wu Y, Zhou Q, Zhao S, Huang X, McCorvy JD, Cai X, Dai A, Roth BL, Hanson MA, Liu ZJ, Wang MW, Stevens RC, Shui W. High-throughput identification of G protein-coupled receptor modulators through affinity mass spectrometry screening. Chem Sci. 2018 Mar 28;9(12):3192-3199. PMCID: PMC5916221 |
32. McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL. Structural determinants of 5-HT<sub>2B</sub> receptor activation and biased agonism. Nat Struct Mol Biol. 2018 Sep;25(9):787-796. PMCID: PMC6237183 |
33. Martini ML, Liu J, Ray C, Yu X, Huang XP, Urs A, Urs N, McCorvy JD, Caron MG, Roth BL, Jin J. Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D<sub>1</sub> Receptor Agonists. J Med Chem. 2019 Apr 11;62(7):3753-3772. PMCID: PMC6688508 |
34. Shen Y, McCorvy JD, Martini ML, Rodriguiz RM, Pogorelov VM, Ward KM, Wetsel WC, Liu J, Roth BL, Jin J. D<sub>2</sub> Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine. J Med Chem. 2019 May 09;62(9):4755-4771. PMCID: PMC6509010 |
35. Stauch B, Johansson LC, McCorvy JD, Patel N, Han GW, Huang XP, Gati C, Batyuk A, Slocum ST, Ishchenko A, Brehm W, White TA, Michaelian N, Madsen C, Zhu L, Grant TD, Grandner JM, Shiriaeva A, Olsen RHJ, Tribo AR, Yous S, Stevens RC, Weierstall U, Katritch V, Roth BL, Liu W, Cherezov V. Structural basis of ligand recognition at the human MT<sub>1</sub> melatonin receptor. Nature. 2019 May;569(7755):284-288. PMCID: PMC6696938 |
36. Johansson LC, Stauch B, McCorvy JD, Han GW, Patel N, Huang XP, Batyuk A, Gati C, Slocum ST, Li C, Grandner JM, Hao S, Olsen RHJ, Tribo AR, Zaare S, Zhu L, Zatsepin NA, Weierstall U, Yous S, Stevens RC, Liu W, Roth BL, Katritch V, Cherezov V. XFEL structures of the human MT<sub>2</sub> melatonin receptor reveal the basis of subtype selectivity. Nature. 2019 May;569(7755):289-292. PMCID: PMC6589158 |
37. Martini ML, Ray C, Yu X, Liu J, Pogorelov VM, Wetsel WC, Huang XP, McCorvy JD, Caron MG, Jin J. Designing Functionally Selective Noncatechol Dopamine D<sub>1</sub> Receptor Agonists with Potent In Vivo Antiparkinsonian Activity. ACS Chem Neurosci. 2019 Sep 18;10(9):4160-4182. PMCID: PMC6785188 |
38. Zhang G, McCorvy JD, Shen S, Cheng J, Roth BL, Kozikowski AP. Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT<sub>2C</sub>) receptor agonist without 5-HT<sub>2B</sub> agonism. Eur J Med Chem. 2019 Nov 15;182:111626. PMCID: PMC6815260 |
39. Sahu BS, Rodriguez P, Nguyen ME, Han R, Cero C, Razzoli M, Piaggi P, Laskowski LJ, Pavlicev M, Muglia L, Mahata SK, O'Grady S, McCorvy JD, Baier LJ, Sham YY, Bartolomucci A. Peptide/Receptor Co-evolution Explains the Lipolytic Function of the Neuropeptide TLQP-21. Cell Rep. 2019 Sep 03;28(10):2567-2580.e6. PMCID: PMC6753381 |
40. Halberstadt AL, Chatha M, Klein AK, McCorvy JD, Meyer MR, Wagmann L, Stratford A, Brandt SD. Pharmacological and biotransformation studies of 1-acyl-substituted derivatives of d-lysergic acid diethylamide (LSD). Neuropharmacology. 2020 Aug 01;172:107856. PMCID: PMC9191647 |
41. Stein RM, Kang HJ, McCorvy JD, Glatfelter GC, Jones AJ, Che T, Slocum S, Huang XP, Savych O, Moroz YS, Stauch B, Johansson LC, Cherezov V, Kenakin T, Irwin JJ, Shoichet BK, Roth BL, Dubocovich ML. Virtual discovery of melatonin receptor ligands to modulate circadian rhythms. Nature. 2020 Mar;579(7800):609-614. PMCID: PMC7134359 |
42. Sherwood AM, Halberstadt AL, Klein AK, McCorvy JD, Kaylo KW, Kargbo RB, Meisenheimer P. Synthesis and Biological Evaluation of Tryptamines Found in Hallucinogenic Mushrooms: Norbaeocystin, Baeocystin, Norpsilocin, and Aeruginascin. J Nat Prod. 2020 Feb 28;83(2):461-467. |
43. Patel N, Huang XP, Grandner JM, Johansson LC, Stauch B, McCorvy JD, Liu Y, Roth B, Katritch V. Structure-based discovery of potent and selective melatonin receptor agonists. Elife. 2020 Mar 02;9. PMCID: PMC7080406 |
44. Olsen RHJ, DiBerto JF, English JG, Glaudin AM, Krumm BE, Slocum ST, Che T, Gavin AC, McCorvy JD, Roth BL, Strachan RT. TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome. Nat Chem Biol. 2020 Aug;16(8):841-849. PMCID: PMC7648517 |
45. Wedemeyer MJ, Mahn SA, Getschman AE, Crawford KS, Peterson FC, Marchese A, McCorvy JD, Volkman BF. The chemokine X-factor: Structure-function analysis of the CXC motif at CXCR4 and ACKR3. J Biol Chem. 2020 Oct 02;295(40):13927-13939. PMCID: PMC7535910 |
46. Cameron LP, Tombari RJ, Lu J, Pell AJ, Hurley ZQ, Ehinger Y, Vargas MV, McCarroll MN, Taylor JC, Myers-Turnbull D, Liu T, Yaghoobi B, Laskowski LJ, Anderson EI, Zhang G, Viswanathan J, Brown BM, Tjia M, Dunlap LE, Rabow ZT, Fiehn O, Wulff H, McCorvy JD, Lein PJ, Kokel D, Ron D, Peters J, Zuo Y, Olson DE. A non-hallucinogenic psychedelic analogue with therapeutic potential. Nature. 2021 Jan;589(7842):474-479. PMCID: PMC7874389 |
47. Klein AK, Chatha M, Laskowski LJ, Anderson EI, Brandt SD, Chapman SJ, McCorvy JD, Halberstadt AL. Investigation of the Structure-Activity Relationships of Psilocybin Analogues. ACS Pharmacol Transl Sci. 2021 Apr 09;4(2):533-542. PMCID: PMC8033608 |
48. Sadler KE, Moehring F, Shiers SI, Laskowski LJ, Mikesell AR, Plautz ZR, Brezinski AN, Mecca CM, Dussor G, Price TJ, McCorvy JD, Stucky CL. Transient receptor potential canonical 5 mediates inflammatory mechanical and spontaneous pain in mice. Sci Transl Med. 2021 May 26;13(595). PMCID: PMC8923002 |
49. Rudin D, McCorvy JD, Glatfelter GC, Luethi D, Szöllősi D, Ljubišić T, Kavanagh PV, Dowling G, Holy M, Jaentsch K, Walther D, Brandt SD, Stockner T, Baumann MH, Halberstadt AL, Sitte HH. (2-Aminopropyl)benzo[β]thiophenes (APBTs) are novel monoamine transporter ligands that lack stimulant effects but display psychedelic-like activity in mice. Neuropsychopharmacology. 2022 Mar;47(4):914-923. PMCID: PMC8882185 |
50. Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL. Structure, function and pharmacology of human itch GPCRs. Nature. 2021 Dec;600(7887):170-175. PMCID: PMC9150435 |
51. Orr MJ, Cao AB, Wang CT, Gaisin A, Csakai A, Friswold AP, Meltzer HY, McCorvy JD, Scheidt KA. Discovery of Highly Potent Serotonin 5-HT<sub>2</sub> Receptor Agonists Inspired by Heteroyohimbine Natural Products. ACS Med Chem Lett. 2022 Apr 14;13(4):648-657. PMCID: PMC9014500 |
52. Kleist AB, Jenjak S, Sente A, Laskowski LJ, Szpakowska M, Calkins MM, Anderson EI, McNally LM, Heukers R, Bobkov V, Peterson FC, Thomas MA, Chevigné A, Smit MJ, McCorvy JD, Babu MM, Volkman BF. Conformational selection guides β-arrestin recruitment at a biased G protein-coupled receptor. Science. 2022 Jul 08;377(6602):222-228. PMCID: PMC9574477 |
53. Fisher CL, Fallot LB, Wan TC, Keyes RF, Suresh RR, Rothwell AC, Gao ZG, McCorvy JD, Smith BC, Jacobson KA, Auchampach JA. Characterization of Dual-Acting A<sub>3</sub> Adenosine Receptor Positive Allosteric Modulators That Preferentially Enhance Adenosine-Induced Gα<sub>i3</sub> and Gα<sub>oA</sub> Isoprotein Activation. ACS Pharmacol Transl Sci. 2022 Aug 12;5(8):625-641. PMCID: PMC9380209 |
54. Kaplan AL, Confair DN, Kim K, Barros-Álvarez X, Rodriguiz RM, Yang Y, Kweon OS, Che T, McCorvy JD, Kamber DN, Phelan JP, Martins LC, Pogorelov VM, DiBerto JF, Slocum ST, Huang XP, Kumar JM, Robertson MJ, Panova O, Seven AB, Wetsel AQ, Wetsel WC, Irwin JJ, Skiniotis G, Shoichet BK, Roth BL, Ellman JA. Bespoke library docking for 5-HT<sub>2A</sub> receptor agonists with antidepressant activity. Nature. 2022 Oct;610(7932):582-591. PMCID: PMC9996387 |
55. Cunningham MJ, Bock HA, Serrano IC, Bechand B, Vidyadhara DJ, Bonniwell EM, Lankri D, Duggan P, Nazarova AL, Cao AB, Calkins MM, Khirsariya P, Hwu C, Katritch V, Chandra SS, McCorvy JD, Sames D. Pharmacological Mechanism of the Non-hallucinogenic 5-HT<sub>2A</sub> Agonist Ariadne and Analogs. ACS Chem Neurosci. 2023 Jan 04;14(1):119-135. PMCID: PMC10147382 |
56. Yahya NA, Lanham JK, Sprague DJ, Palygin O, McCorvy JD, Marchant JS. Molecular and cellular basis of praziquantel action in the cardiovascular system. Am J Physiol Cell Physiol. 2023 Feb 01;324(2):C573-C587. PMCID: PMC9942900 |
57. Elmansi AM, Eisa NH, Periyasamy-Thandavan S, Kondrikova G, Kondrikov D, Calkins MM, Aguilar-Pérez A, Chen J, Johnson M, Shi XM, Reitman C, McGee-Lawrence ME, Crawford KS, Dwinell MB, Volkman BF, Blumer JB, Luttrell LM, McCorvy JD, Hill WD. DPP4-Truncated CXCL12 Alters CXCR4/ACKR3 Signaling, Osteogenic Cell Differentiation, Migration, and Senescence. ACS Pharmacol Transl Sci. 2023 Jan 13;6(1):22-39. PMCID: PMC9844133 |
58. Vargas MV, Dunlap LE, Dong C, Carter SJ, Tombari RJ, Jami SA, Cameron LP, Patel SD, Hennessey JJ, Saeger HN, McCorvy JD, Gray JA, Tian L, Olson DE. Psychedelics promote neuroplasticity through the activation of intracellular 5-HT2A receptors. Science. 2023 Feb 17;379(6633):700-706. PMCID: PMC10108900 |
59. Lewis V, Bonniwell EM, Lanham JK, Ghaffari A, Sheshbaradaran H, Cao AB, Calkins MM, Bautista-Carro MA, Arsenault E, Telfer A, Taghavi-Abkuh FF, Malcolm NJ, El Sayegh F, Abizaid A, Schmid Y, Morton K, Halberstadt AL, Aguilar-Valles A, McCorvy JD. A non-hallucinogenic LSD analog with therapeutic potential for mood disorders. Cell Rep. 2023 Mar 28;42(3):112203. PMCID: PMC10112881 |
60. Malcolm NJ, Palkovic B, Sprague DJ, Calkins MM, Lanham JK, Halberstadt AL, Stucke AG, McCorvy JD. Mu-opioid receptor selective superagonists produce prolonged respiratory depression. iScience. 2023 Jul 21;26(7):107121. PMCID: PMC10320493 |
61. Balapattabi K, Yavuz Y, Jiang J, Deng G, Mathieu NM, Ritter ML, Opichka MA, Reho JJ, McCorvy JD, Nakagawa P, Morselli LL, Mouradian GC Jr, Atasoy D, Cui H, Hodges MR, Sigmund CD, Grobe JL. Angiotensin AT<sub>1A</sub> receptor signal switching in Agouti-related peptide neurons mediates metabolic rate adaptation during obesity. Cell Rep. 2023 Aug 29;42(8):112935. PMCID: PMC10530419 |
62. Tosh DK, Calkins MM, Ivancich MS, Bock HA, Campbell RG, Lewicki SA, Chen E, Gao ZG, McCorvy JD, Jacobson KA. Structure activity relationships of 5-HT<sub>2B</sub> and 5-HT<sub>2C</sub> serotonin receptor antagonists: N<sup>6</sup>, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives. Eur J Med Chem. 2023 Nov 05;259:115691. PMCID: PMC10529765 |
63. Wallach J, Cao AB, Calkins MM, Heim AJ, Lanham JK, Bonniwell EM, Hennessey JJ, Bock HA, Anderson EI, Sherwood AM, Morris H, de Klein R, Klein AK, Cuccurazzu B, Gamrat J, Fannana T, Zauhar R, Halberstadt AL, McCorvy JD. Identification of 5-HT<sub>2A</sub> Receptor Signaling Pathways Responsible for Psychedelic Potential. bioRxiv. 2023 Jul 31. PMCID: PMC10418054 |
64. Kelly TJ, Bonniwell EM, Mu L, Liu X, Hu Y, Friedman V, Yu H, Su W, McCorvy JD, Liu QS. Psilocybin analog 4-OH-DiPT enhances fear extinction and GABAergic inhibition of principal neurons in the basolateral amygdala. Neuropsychopharmacology. 2024 Apr;49(5):854-863. PMCID: PMC10948882 |
65. Cameron LP, Benetatos J, Lewis V, Bonniwell EM, Jaster AM, Moliner R, Castrén E, McCorvy JD, Palner M, Aguilar-Valles A. Beyond the 5-HT<sub>2A</sub> Receptor: Classic and Nonclassic Targets in Psychedelic Drug Action. J Neurosci. 2023 Nov 08;43(45):7472-7482. PMCID: PMC10634557 |
66. Rodriguez P, Laskowski LJ, Pallais JP, Bock HA, Cavalco NG, Anderson EI, Calkins MM, Razzoli M, Sham YY, McCorvy JD, Bartolomucci A. Functional profiling of the G protein-coupled receptor C3aR1 reveals ligand-mediated biased agonism. J Biol Chem. 2024 Jan;300(1):105549. PMCID: PMC10796979 |
67. Wallach J, Cao AB, Calkins MM, Heim AJ, Lanham JK, Bonniwell EM, Hennessey JJ, Bock HA, Anderson EI, Sherwood AM, Morris H, de Klein R, Klein AK, Cuccurazzu B, Gamrat J, Fannana T, Zauhar R, Halberstadt AL, McCorvy JD. Identification of 5-HT<sub>2A</sub> receptor signaling pathways associated with psychedelic potential. Nat Commun. 2023 Dec 15;14(1):8221. PMCID: PMC10724237 |
68. Schlimgen RR, Peterson FC, Heukers R, Smit MJ, McCorvy JD, Volkman BF. Structural basis for selectivity and antagonism in extracellular GPCR-nanobodies. Nat Commun. 2024 May 30;15(1):4611. PMCID: PMC11139983 |
69. Alberto-Silva AS, Hemmer S, Bock HA, Alves da Silva L, Scott KR, Kastner N, Bhatt M, Niello M, Jäntsch K, Kudlacek O, Bossi E, Stockner T, Meyer MR, McCorvy JD, Brandt SD, Kavanagh P, Sitte HH. Bioisosteric analogs of MDMA with improved pharmacological profile. bioRxiv. 2024 Apr 11. PMCID: PMC11030374 |
70. Alberto-Silva AS, Hemmer S, Bock HA, da Silva LA, Scott KR, Kastner N, Bhatt M, Niello M, Jäntsch K, Kudlacek O, Bossi E, Stockner T, Meyer MR, McCorvy JD, Brandt SD, Kavanagh P, Sitte HH. Bioisosteric analogs of MDMA: Improving the pharmacological profile? J Neurochem. 2024 Sep;168(9):2022-2042. PMCID: PMC11449655 |
71. Denomme N, Hernandez CC, Bock HA, Ohana RF, Bakshi S, Sherwood AM, McCorvy JD, Daley PF, Callaway WB, Hull JM, Alt A, Isom LL, Cozzi NV. <i>N</i>-(4-Bromo-2,5-Dimethoxyphenethyl)-6-(4-Phenylbutoxy)Hexan-1-Amine (XOB): A Novel Phenylalkylamine Antagonist of Serotonin 2A Receptors and Voltage-Gated Sodium Channels. Mol Pharmacol. 2024 Jul 17;106(2):92-106. PMCID: PMC11254453 |
72. Tosh DK, Calkins MM, Ivancich MS, Bock HA, Campbell RG, Lewicki SA, Chen E, Gao ZG, McCorvy JD, Jacobson KA. Structure activity relationships of 5-HT<inf>2B</inf> and 5-HT<inf>2C</inf> serotonin receptor antagonists: N<sup>6</sup>, C2 and 5′-Modified (N)-methanocarba-adenosine derivatives European Journal of Medicinal Chemistry. 5 November 2023;259. |
Books, Chapters, and Reviews |
1. McCorvy JD, Roth BL. Structure and function of serotonin G protein-coupled receptors. Pharmacol Ther. 2015 Jun;150:129-42. PMCID: PMC4414735 |
2. McCorvy JD, Olsen RH, Roth BL. Psilocybin for depression and anxiety associated with life-threatening illnesses. J Psychopharmacol. 2016 Dec;30(12):1209-1210. |
3. Tan L, Yan W, McCorvy JD, Cheng J. Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. J Med Chem. 2018 Nov 21;61(22):9841-9878. |
4. Sanchez-Reyes OB, Zilberg G, McCorvy JD, Wacker D. Molecular insights into GPCR mechanisms for drugs of abuse. J Biol Chem. 2023 Sep;299(9):105176. PMCID: PMC10514560 |
