P
Patrick M. Giguère
Researcher at University of North Carolina at Chapel Hill
Publications - 44
Citations - 3211
Patrick M. Giguère is an academic researcher from University of North Carolina at Chapel Hill. The author has contributed to research in topics: G protein-coupled receptor & G protein. The author has an hindex of 22, co-authored 36 publications receiving 2667 citations. Previous affiliations of Patrick M. Giguère include Université de Sherbrooke.
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Structure-based discovery of opioid analgesics with reduced side effects
Aashish Manglik,Henry Lin,Dipendra K. Aryal,John D. McCorvy,Daniela Dengler,Gregory Corder,Anat Levit,Ralf C. Kling,Ralf C. Kling,Viachaslau Bernat,Harald Hübner,Xi Ping Huang,Maria F. Sassano,Patrick M. Giguère,Stefan Löber,Da Duan,Grégory Scherrer,Brian K. Kobilka,Peter Gmeiner,Bryan L. Roth,Brian K. Shoichet +20 more
TL;DR: PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment and is devoid of both respiratory depression and morphine-like reinforcing activity in mice at equi-analgesic doses.
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PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome
Wesley K. Kroeze,Maria F. Sassano,Xi Ping Huang,Katherine Lansu,John D. McCorvy,Patrick M. Giguère,Noah Sciaky,Bryan L. Roth +7 more
TL;DR: A unique open-source resource is described that allows interrogation of the druggable human GPCRome via a G protein–independent β-arrestin–recruitment assay and its utility for discovering new ligands for orphanhuman GPCRs is demonstrated.
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Molecular control of δ-opioid receptor signalling
Gustavo Fenalti,Patrick M. Giguère,Vsevolod Katritch,Xi Ping Huang,Aaron Thompson,Vadim Cherezov,Bryan L. Roth,Raymond C. Stevens +7 more
TL;DR: The data establish the molecular basis for allosteric sodium ion control in opioid signalling, revealing that sodium-coordinating residues act as ‘efficacy switches’ at a prototypic G-protein-coupled receptor.
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A New DREADD Facilitates the Multiplexed Chemogenetic Interrogation of Behavior
Eyal Vardy,J. Elliott Robinson,Chia Li,Chia Li,Reid H.J. Olsen,Jeffrey F. DiBerto,Patrick M. Giguère,Flori M. Sassano,Xi Ping Huang,Hu Zhu,Daniel J. Urban,Kate L. White,Joseph E. Rittiner,Nicole A. Crowley,Kristen E. Pleil,Christopher M. Mazzone,Philip D. Mosier,Juan Song,Thomas L. Kash,C. J. Malanga,Michael J. Krashes,Michael J. Krashes,Bryan L. Roth +22 more
TL;DR: A structure-based approach is used to develop a new Gi-coupled DREADD using the kappa-opioid receptor as a template that is activated by the pharmacologically inert ligand salvinorin B (SALB) that robustly attenuated neuronal activity and modified behaviors.
Journal ArticleDOI
The Mitochondrial Proteins NLRX1 and TUFM Form a Complex that Regulates Type I Interferon and Autophagy
Yu Lei,Haitao Wen,Yanbao Yu,Debra J. Taxman,Lu Zhang,Douglas G. Widman,Karen V. Swanson,Kwun Wah Wen,Blossom Damania,Christopher Brooks Moore,Patrick M. Giguère,David P. Siderovski,John Hiscott,Babak Razani,Clay F. Semenkovich,Xian Chen,Jenny P.-Y. Ting +16 more
TL;DR: This study establishes a link between an NLR protein and the viral-induced autophagic machinery via an intermediary partner, TUFM, which has similar functions as NLRX1 by inhibiting RLR-induced IFN-I but promoting autophagy.