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Uncovering molecular mechanisms involved in activation of G protein-coupled receptors.
G protein-coupled, seven-transmembrane segment receptors (GPCRs or 7TM receptors), with more than 1000 different members, comprise the largest superfamily of proteins in the body. Since the cloning of the first receptors more than a decade ago, extensive
U. Gether
semanticscholar +1 more source
G Protein–Coupled Receptor Deorphanizations [PDF]
G protein–coupled receptors (GPCRs) are major regulators of intercellular interactions. They initiate these actions by being activated by a wide variety of natural ligands. Historically, ligands were discovered first, but the advent of molecular biology reversed this trend.
Zhiwei Wang+5 more
openaire +3 more sources
Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells
G protein–coupled receptors (GPCRs) are key signaling proteins that regulate nearly every aspect of cell function. Studies of GPCRs have benefited greatly from the development of molecular tools to monitor receptor activation and downstream signaling ...
Qingwen Wan+6 more
semanticscholar +1 more source
G protein-coupled receptors are 7-pass transmembrane receptors that couple to heterotrimeric G proteins to mediate cellular responses to a diverse array of stimuli.
Alexander Bowitch+3 more
doaj +1 more source
THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: G protein‐coupled receptors
The Concise Guide to PHARMACOLOGY 2017/18 provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to an open access knowledgebase of drug targets and ...
Stephen P. H. Alexander+11 more
semanticscholar +1 more source
G Protein‐Coupled receptors and heterotrimeric G proteins as cancer drivers
G protein‐coupled receptors (GPCRs) and heterotrimeric G proteins play central roles in a diverse array of cellular processes. As such, dysregulation of GPCRs and their coupled heterotrimeric G proteins can dramatically alter the signalling landscape and
Nadia Arang, J. Gutkind
semanticscholar +1 more source
Powdered G-Protein-Coupled Receptors [PDF]
Preparation and storage of functional membrane proteins such as G-protein-coupled receptors (GPCRs) are crucial to the processes of drug delivery and discovery. Here, we describe a method of preparing powdered GPCRs using rhodopsin as the prototype. We purified rhodopsin in CHAPS detergent with low detergent to protein ratio so the bulk of the sample ...
Suchithranga M. D. C. Perera+2 more
openaire +3 more sources
Fusion protein strategies for cryo-EM study of G protein-coupled receptors
Here, Zhang et al. explore fusion protein strategies to facilitate cryo-EM structural studies of GPCRs alone- without signal transducers- in ligand bound or unliganded form.
Kaihua Zhang+4 more
doaj +1 more source
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 represent one of the largest class of surface receptors targeted by drugs.
Jialu Wang, C. Gareri, H. Rockman
semanticscholar +1 more source
Rules and mechanisms governing G protein coupling selectivity of GPCRs
Summary: G protein-coupled receptors (GPCRs) convert extracellular stimuli into intracellular signaling by coupling to heterotrimeric G proteins of four classes: Gi/o, Gq, Gs, and G12/13.
Ikuo Masuho+8 more
doaj