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 …

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 …

[HTML][HTML] Illuminating G-protein-coupling selectivity of GPCRs

A Inoue, F Raimondi, FMN Kadji, G Singh, T Kishi… - Cell, 2019 - cell.com
Heterotrimetic G proteins consist of four subfamilies (G s, G i/o, G q/11, and G 12/13) that
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …

[HTML][HTML] Pharmacogenomics of GPCR drug targets

AS Hauser, S Chavali, I Masuho, LJ Jahn… - Cell, 2018 - cell.com
Natural genetic variation in the human genome is a cause of individual differences in
responses to medications and is an underappreciated burden on public health. Although …

The contribution of intrinsically disordered regions to protein function, cellular complexity, and human disease

MM Babu - Biochemical Society Transactions, 2016 - portlandpress.com
In the 1960s, Christian Anfinsen postulated that the unique three-dimensional structure of a
protein is determined by its amino acid sequence. This work laid the foundation for the …

GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures

I Shimada, T Ueda, Y Kofuku, MT Eddy… - Nature Reviews Drug …, 2019 - nature.com
The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …

Autoregulation of GPCR signalling through the third intracellular loop

F Sadler, N Ma, M Ritt, Y Sharma, N Vaidehi… - Nature, 2023 - nature.com
The third intracellular loop (ICL3) of the G protein-coupled receptor (GPCR) fold is important
for the signal transduction process downstream of receptor activation,–. Despite this, the lack …

Diverse activation pathways in class A GPCRs converge near the G-protein-coupling region

AJ Venkatakrishnan, X Deupi, G Lebon… - Nature, 2016 - nature.com
Class A G-protein-coupled receptors (GPCRs) are a large family of membrane proteins that
mediate a wide variety of physiological functions, including vision, neurotransmission and …

How phosphorylation impacts intrinsically disordered proteins and their function

EA Newcombe, E Delaforge… - Essays in …, 2022 - portlandpress.com
Phosphorylation is the most common post-translational modification (PTM) in eukaryotes,
occurring particularly frequently in intrinsically disordered proteins (IDPs). These proteins …

Combinatorial expression of GPCR isoforms affects signalling and drug responses

M Marti-Solano, SE Crilly, D Malinverni, C Munk… - Nature, 2020 - nature.com
G-protein-coupled receptors (GPCRs) are membrane proteins that modulate physiology
across human tissues in response to extracellular signals. GPCR-mediated signalling can …