G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

Impact of GPCR structures on drug discovery

M Congreve, C de Graaf, NA Swain, CG Tate - Cell, 2020 - cell.com
Structures of 70 unique G protein-coupled receptors (GPCRs) have been determined, with
over 370 structures in total bound to different ligands and the receptors in various …

Structure, function and pharmacology of human itch GPCRs

C Cao, HJ Kang, I Singh, H Chen, C Zhang, W Ye… - Nature, 2021 - nature.com
The MRGPRX family of receptors (MRGPRX1–4) is a family of mas-related G-protein-
coupled receptors that have evolved relatively recently. Of these, MRGPRX2 and MRGPRX4 …

Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

RCSB Protein Data Bank: Enabling biomedical research and drug discovery

DS Goodsell, C Zardecki, L Di Costanzo… - Protein …, 2020 - Wiley Online Library
Analyses of publicly available structural data reveal interesting insights into the impact of the
three‐dimensional (3D) structures of protein targets important for discovery of new drugs …

GPCR dynamics: structures in motion

NR Latorraca, AJ Venkatakrishnan, RO Dror - Chemical reviews, 2017 - ACS Publications
The function of G protein-coupled receptors (GPCRs) which represent the largest class of
both human membrane proteins and drug targets depends critically on their ability to …

Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone

S Wang, T Che, A Levit, BK Shoichet, D Wacker… - Nature, 2018 - nature.com
Dopamine is a neurotransmitter that has been implicated in processes as diverse as reward,
addiction, control of coordinated movement, metabolism and hormonal secretion …

Structural insights into µ-opioid receptor activation

W Huang, A Manglik, AJ Venkatakrishnan… - Nature, 2015 - nature.com
Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …

Structure of the adenosine-bound human adenosine A1 receptor–Gi complex

CJ Draper-Joyce, M Khoshouei, DM Thal, YL Liang… - Nature, 2018 - nature.com
The class A adenosine A1 receptor (A1R) is a G-protein-coupled receptor that preferentially
couples to inhibitory Gi/o heterotrimeric G proteins, has been implicated in numerous …

The molecular basis of G protein–coupled receptor activation

WI Weis, BK Kobilka - Annual review of biochemistry, 2018 - annualreviews.org
G protein–coupled receptors (GPCRs) mediate the majority of cellular responses to external
stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein …