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 …
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
Impact of GPCR structures on drug discovery
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 …
over 370 structures in total bound to different ligands and the receptors in various …
Structure, function and pharmacology of human itch GPCRs
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 …
coupled receptors that have evolved relatively recently. Of these, MRGPRX2 and MRGPRX4 …
Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …
RCSB Protein Data Bank: Enabling biomedical research and drug discovery
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 …
three‐dimensional (3D) structures of protein targets important for discovery of new drugs …
GPCR dynamics: structures in motion
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 …
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
Dopamine is a neurotransmitter that has been implicated in processes as diverse as reward,
addiction, control of coordinated movement, metabolism and hormonal secretion …
addiction, control of coordinated movement, metabolism and hormonal secretion …
Structural insights into µ-opioid receptor activation
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 …
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
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 …
couples to inhibitory Gi/o heterotrimeric G proteins, has been implicated in numerous …
The molecular basis of G protein–coupled receptor activation
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 …
stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein …