Mechanisms of signalling and biased agonism in G protein-coupled receptors
D Wootten, A Christopoulos, M Marti-Solano… - … reviews Molecular cell …, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest group of cell surface receptors in
humans that signal in response to diverse inputs and regulate a plethora of cellular …
humans that signal in response to diverse inputs and regulate a plethora of cellular …
Structure and dynamics of GPCR signaling complexes
G-protein-coupled receptors (GPCRs) relay numerous extracellular signals by triggering
intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs …
intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs …
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 …
GPCR activation mechanisms across classes and macro/microscales
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
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 …
Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia
The adenosine A1 receptor (A1R) is a promising therapeutic target for non-opioid analgesic
agents to treat neuropathic pain,. However, development of analgesic orthosteric A1R …
agents to treat neuropathic pain,. However, development of analgesic orthosteric A1R …
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 …
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 …
Discovering Anti-Cancer Drugs via Computational Methods
New drug discovery has been acknowledged as a complicated, expensive, time-consuming,
and challenging project. It has been estimated that around 12 years and 2.7 billion USD, on …
and challenging project. It has been estimated that around 12 years and 2.7 billion USD, on …
Nanodiscs in membrane biochemistry and biophysics
IG Denisov, SG Sligar - Chemical reviews, 2017 - ACS Publications
Membrane proteins play a most important part in metabolism, signaling, cell motility,
transport, development, and many other biochemical and biophysical processes which …
transport, development, and many other biochemical and biophysical processes which …