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 …
G-protein–coupled receptors in heart disease
GPCRs (G-protein [guanine nucleotide-binding protein]–coupled receptors) play a central
physiological role in the regulation of cardiac function in both health and disease and thus …
physiological role in the regulation of cardiac function in both health and disease and thus …
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 …
Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
S Lu, X He, Z Yang, Z Chai, S Zhou, J Wang… - Nature …, 2021 - nature.com
G protein-coupled receptors (GPCRs) are the most common proteins targeted by approved
drugs. A complete mechanistic elucidation of large-scale conformational transitions …
drugs. A complete mechanistic elucidation of large-scale conformational transitions …
Multiscale simulations of biological membranes: the challenge to understand biological phenomena in a living substance
Biological membranes are tricky to investigate. They are complex in terms of molecular
composition and structure, functional over a wide range of time scales, and characterized by …
composition and structure, functional over a wide range of time scales, and characterized by …
Structural insights into G-protein-coupled receptor allostery
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …
PtdIns (4, 5) P2 stabilizes active states of GPCRs and enhances selectivity of G-protein coupling
G-protein-coupled receptors (GPCRs) are involved in many physiological processes and are
therefore key drug targets 1. Although detailed structural information is available for GPCRs …
therefore key drug targets 1. Although detailed structural information is available for GPCRs …
Small-molecule discovery through DNA-encoded libraries
AA Peterson, DR Liu - Nature Reviews Drug Discovery, 2023 - nature.com
The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …
discovery platforms that enable access to chemical diversity and can quickly reveal new …
A µ-opioid receptor modulator that works cooperatively with naloxone
The µ-opioid receptor (µOR) is a well-established target for analgesia, yet conventional
opioid receptor agonists cause serious adverse effects, notably addiction and respiratory …
opioid receptor agonists cause serious adverse effects, notably addiction and respiratory …
The pocketome of G-protein-coupled receptors reveals previously untargeted allosteric sites
JB Hedderich, M Persechino, K Becker… - Nature …, 2022 - nature.com
G-protein-coupled receptors do not only feature the orthosteric pockets, where most
endogenous agonists bind, but also a multitude of other allosteric pockets that have come …
endogenous agonists bind, but also a multitude of other allosteric pockets that have come …