P
Peter Gmeiner
Researcher at University of Erlangen-Nuremberg
Publications - 387
Citations - 10910
Peter Gmeiner is an academic researcher from University of Erlangen-Nuremberg. The author has contributed to research in topics: Agonist & Receptor. The author has an hindex of 46, co-authored 378 publications receiving 9632 citations. Previous affiliations of Peter Gmeiner include Innsbruck Medical University & UCB.
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Journal ArticleDOI
Activation and allosteric modulation of a muscarinic acetylcholine receptor
Andrew C. Kruse,Aaron M. Ring,Aashish Manglik,Jianxin Hu,Kelly Hu,Katrin Eitel,Harald Hübner,Els Pardon,Celine Valant,Patrick M. Sexton,Arthur Christopoulos,Christian C. Felder,Peter Gmeiner,Jan Steyaert,William I. Weis,K. Christopher Garcia,Jürgen Wess,Brian K. Kobilka +17 more
TL;DR: The structure of an agonist-bound, active state of the human M2 muscarinic acetylcholine receptor stabilized by a G-protein mimetic camelid antibody fragment isolated by conformational selection using yeast surface display reveals larger conformational changes in the extracellular region and orthosteric binding site than observed in the active states of the β2AR and rhodopsin.
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Structure and function of an irreversible agonist-β2 adrenoceptor complex
Daniel M. Rosenbaum,Cheng Zhang,Joseph A. Lyons,Joseph A. Lyons,Ralph Holl,David Aragão,Daniel H. Arlow,Sã̧ren G F Rasmussen,Hee Jung Choi,Brian T. DeVree,Roger K. Sunahara,Pil Seok Chae,Samuel H. Gellman,Ron O. Dror,David E. Shaw,William I. Weis,Martin Caffrey,Peter Gmeiner,Brian K. Kobilka +18 more
TL;DR: A covalent agonist-bound β2AR–T4L fusion protein is designed that can be covalently tethered to a specific site on the receptor through a disulphide bond, and is capable of activating a heterotrimeric G protein.
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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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Structural insights into µ-opioid receptor activation
Weijiao Huang,Aashish Manglik,AJ Venkatakrishnan,Toon Laeremans,Evan N. Feinberg,Adrian L. Sanborn,Hideaki E. Kato,Kathryn E. Livingston,Thor S. Thorsen,Ralf C. Kling,Sébastien Granier,Peter Gmeiner,Stephen M. Husbands,John R. Traynor,William I. Weis,Jan Steyaert,Ron O. Dror,Brian K. Kobilka +17 more
TL;DR: A 2.1 Å X-ray crystal structure of the murine μOR bound to the morphinan agonist BU72 and a G protein mimetic camelid antibody fragment is reported, revealing an extensive polar network between the ligand-binding pocket and the cytoplasmic domains appears to play a similar role in signal propagation for all three G-protein-coupled receptors.
Journal ArticleDOI
Interactive SAR Studies: Rational Discovery of Super-Potent and Highly Selective Dopamine D3 Receptor Antagonists and Partial Agonists
TL;DR: An interactive drug discovery process leading to heterocyclic bioisosteres is demonstrated and the benzothiophenes 3c and 3d revealed outstanding D3 affinity and subtype selectivity.