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REGA-SIGN: Development of a Novel Set of NanoBRET-Based G Protein Biosensors
Despite G protein-coupled receptors (GPCRs) being important theapeutic targets, the signaling properties of many GPCRs remain poorly characterized. GPCR activation primarily initiates heterotrimeric G protein signaling. To detect ligand-induced G protein
Katrijn Boon +4 more
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Multi-Omics Analysis of Multiple Glucose-Sensing Receptor Systems in Yeast
The yeast Saccharomyces cerevisiae has long been used to produce alcohol from glucose and other sugars. While much is known about glucose metabolism, relatively little is known about the receptors and signaling pathways that indicate glucose availability.
Shuang Li +7 more
doaj +1 more source
Multiple endocytic pathways of G protein-coupled receptors delineated by GIT1 sensitivity. [PDF]
Recently, we identified a GTPase-activating protein for the ADP ribosylation factor family of small GTP-binding proteins that we call GIT1. This protein initially was identified as an interacting partner for the G protein-coupled receptor kinases, and ...
Achiriloaie, M +6 more
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Aims/Introduction Incretin hormone glucose‐dependent insulinotropic polypeptide/gastric inhibitory polypeptide (GIP) plays a key role in high‐fat diet‐induced obesity and insulin resistance.
Akiko Sankoda +8 more
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Receptor Quaternary Organization Explains G Protein-Coupled Receptor Family Structure
The organization of Rhodopsin-family G protein-coupled receptors (GPCRs) at the cell surface is controversial. Support both for and against the existence of dimers has been obtained in studies of mostly individual receptors.
James H. Felce +7 more
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Cryo‐EM structure of G‐protein‐coupled receptor GPR17 in complex with inhibitory G protein
GPR17 is a class A orphan G protein‐coupled receptor (GPCR) expressed in neurons and oligodendrocyte progenitors of the central nervous system (CNS). The signalling of GPR17 occurs through the heterotrimeric Gi, but its activation mechanism is unclear ...
Fang Ye +10 more
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G PROTEIN–COUPLED RECEPTOR KINASES [PDF]
G protein–coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein–coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization.
J A, Pitcher +2 more
openaire +2 more sources
Competing G protein‐coupled receptor kinases balance G protein and β‐arrestin signaling
Seven‐transmembrane receptors (7TMRs) are involved in nearly all aspects of chemical communications and represent major drug targets. 7TMRs transmit their signals not only via heterotrimeric G proteins but also through β‐arrestins, whose recruitment to ...
Domitille Heitzler +15 more
doaj +1 more source
The regulatory role of estrogens and nuclear estrogen receptors, i. e., estrogen receptor α and β has been reported in gastrointestinal diseases. However, the contribution of G protein-coupled estrogen receptor, the membrane-bound estrogen receptor, is ...
Damian Jacenik, Wanda M. Krajewska
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Molecular mechanism of Gαi activation by non-GPCR proteins with a Gα-Binding and Activating motif [PDF]
Heterotrimeric G proteins are quintessential signalling switches activated by nucleotide exchange on Gα. Although activation is predominantly carried out by G-protein-coupled receptors (GPCRs), non-receptor guanine-nucleotide exchange factors (GEFs) have
Baillie, George S. +14 more
core +1 more source

