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 …

Biased signalling: from simple switches to allosteric microprocessors

JS Smith, RJ Lefkowitz, S Rajagopal - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …

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 …

Into the tissues: Extracellular matrix and its artificial substitutes: Cell signalling mechanisms

A Bandzerewicz, A Gadomska-Gajadhur - Cells, 2022 - mdpi.com
The existence of orderly structures, such as tissues and organs is made possible by cell
adhesion, ie, the process by which cells attach to neighbouring cells and a supporting …

Microbial and animal rhodopsins: structures, functions, and molecular mechanisms

OP Ernst, DT Lodowski, M Elstner, P Hegemann… - Chemical …, 2014 - ACS Publications
Organisms of all domains of life use photoreceptor proteins to sense and respond to light.
The light-sensitivity of photoreceptor proteins arises from bound chromophores such as …

Molecular signatures of G-protein-coupled receptors

AJ Venkatakrishnan, X Deupi, G Lebon, CG Tate… - Nature, 2013 - nature.com
G-protein-coupled receptors (GPCRs) are physiologically important membrane proteins that
sense signalling molecules such as hormones and neurotransmitters, and are the targets of …

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

WK Kroeze, MF Sassano, XP Huang, K Lansu… - Nature structural & …, 2015 - nature.com
G protein–coupled receptors (GPCRs) are essential mediators of cellular signaling and are
important targets of drug action. Of the approximately 350 nonolfactory human GPCRs, more …

Roles of Mas-related G protein–coupled receptor X2 on mast cell–mediated host defense, pseudoallergic drug reactions, and chronic inflammatory diseases

H Subramanian, K Gupta, H Ali - Journal of Allergy and Clinical …, 2016 - Elsevier
Mast cells (MCs), which are granulated tissue-resident cells of hematopoietic lineage,
contribute to vascular homeostasis, innate/adaptive immunity, and wound healing. However …

Adenosine receptors as drug targets—what are the challenges?

JF Chen, HK Eltzschig, BB Fredholm - Nature reviews Drug discovery, 2013 - nature.com
Adenosine signalling has long been a target for drug development, with adenosine itself or
its derivatives being used clinically since the 1940s. In addition, methylxanthines such as …

Structure-function of the G protein–coupled receptor superfamily

V Katritch, V Cherezov… - Annual review of …, 2013 - annualreviews.org
During the past few years, crystallography of G protein–coupled receptors (GPCRs) has
experienced exponential growth, resulting in the determination of the structures of 16 distinct …