Results 51 to 60 of about 6,551 (208)

The potential for biased signalling in the P2Y receptor family of GPCRs

open access: yesBritish Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk   +2 more
wiley   +1 more source

GRK2 is directly targeted by miR-K3.

open access: yes, 2015
(A). Luciferase activity was detected in HEK 293T cells co-transfected by a mimic of miR-K3 (miR-K3) or a negative control nucleotide of miRNA (Neg. Ctrl.) together with pGL3-Control or pGL3-GRK2 3’UTR luciferase reporter (pGL3-GRK2 3’UTR).
Di Qin (107446)   +11 more
core   +1 more source

Diseño racional de inhibidores de la actividad RGS de GRK2 [PDF]

open access: yes, 2018
GRK2 overexpression is involved in the development of several pathologies with unsatisfied therapeutic demand. Plenty evidences demonstrate a desensitizating mechanism for GPCRs, associated to GRK2 RGS homology domain, and independent of its kinase ...
Echeverría, Emiliana
core   +2 more sources

Sex Differences in High Fat Diet-Induced Metabolic Alterations Correlate with Changes in the Modulation of GRK2 Levels

open access: yesCells, 2019
A differential sex-related sensitivity has been reported in obesity and insulin resistance-related cardio-metabolic diseases, with a lower incidence of these pathologies being observed in young females when compared to age-matched males.
Alba C. Arcones   +4 more
doaj   +1 more source

The c‐Src inhibitor eCF506 diminishes opioid tolerance and reduces β‐arrestin2 recruitment

open access: yesBritish Journal of Pharmacology, EarlyView.
Morphine activation of μ receptors causes tolerance through c‐Src activation and β‐arrestin2 recruitment. c‐Src inhibition or degradation reduces β‐arrestin2 recruitment, μ receptor endocytosis, while causing receptor upregulation, all likely contributing to reduced morphine tolerance.
Samuel Singleton   +6 more
wiley   +1 more source

GRK2 contributes to glucose mediated calcium responses and insulin secretion in pancreatic islet cells

open access: yesScientific Reports, 2021
Diabetes is a metabolic syndrome rooted in impaired insulin and/or glucagon secretory responses within the pancreatic islets of Langerhans (islets).
Jonathan Snyder   +5 more
doaj   +1 more source

Broadening horizons: Pathogenesis and therapeutics of renal ciliopathies

open access: yesJournal of Cell Communication and Signaling, Volume 20, Issue 3, September 2026.
This review elucidates the molecular mechanisms and aberrant signaling pathways in renal ciliopathies, links genetic heterogeneity to clinical phenotypes, and lays a theoretical basis for prenatal diagnosis and novel therapies. Abstract Renal ciliopathies encompass a spectrum of genetic disorders arising from structural or functional impairments of ...
Qiaowei Zhang   +7 more
wiley   +1 more source

Overexpression of GRK2 in vascular smooth muscle leads to inappropriate hypertension and acute heart failure as in clinical scenario 1

open access: yesScientific Reports, 2023
Clinical scenario 1 (CS1) is acute heart failure (HF) characterized by transient systolic blood pressure (SBP) elevation and pulmonary congestion. Although it is managed by vasodilators, the molecular mechanism remains unclear.
Hiroki Yano   +12 more
doaj   +1 more source

Unraveling the Anti‐Arthritic Potential of Bioactive Compounds From Melaleuca alternifolia Oil: Integrated In Vivo, Molecular Docking, and Network Pharmacology Insights

open access: yesFood Science &Nutrition, Volume 14, Issue 9, September 2026.
Melaleuca alternifolia oil demonstrated significant anti‐arthritic effects in CFA‐induced rats by reducing paw edema, PGE2 levels, and inflammatory biomarkers. It improved hematological and histopathological parameters, modulated cytokine expression, and showed promising phytochemical‐target interactions through GC–MS, network pharmacology, and ...
Sana Sabir   +15 more
wiley   +1 more source

G protein-coupled receptor kinase 2-mediated phosphorylation of ezrin is required for G protein-coupled receptor-dependent reorganization of the actin cytoskeleton [PDF]

open access: yes, 2005
G protein-coupled receptor kinase 2 (GRK2) phosphorylates and desensitizes activated G protein-coupled receptors (GPCRs). Here, we identify ezrin as a novel non-GPCR substrate of GRK2. GRK2 phosphorylates glutathione S-transferase (GST)-ezrin, but not an
Pitcher, JA, Cant, SH
core  

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