Rate of Homologous Desensitization and Internalization of the GLP-1 Receptor [PDF]
Molecules, 2016 The glucagon-like peptide-1 receptor (GLP-1R) is an important target in the treatment of type 2 diabetes mellitus. The aim of this study was to compare the rate of agonist stimulated desensitization and internalization of GLP-1R.
Ghina Shaaban +2 more
doaj +5 more sources
The Regulator of G Protein Signaling Homologous Domain of G Protein-Coupled Receptor Kinase 2 Mediates Short-Term Desensitization of β3-Adrenergic Receptor [PDF]
Frontiers in Pharmacology, 2020 G protein coupled receptor (GPCR) kinases (GRKs) are key regulators of GPCR signaling. Canonical mechanism of GPCR desensitization involves receptor phosphorylation by GRKs followed by arrestin recruitment and uncoupling from heterotrimeric G protein ...
Emiliana Echeverría +18 more
doaj +2 more sources
Calcineurin regulates homologous desensitization of natriuretic peptide receptor-A and inhibits ANP-induced testosterone production in MA-10 cells. [PDF]
PLoS ONE, 2012 Receptor desensitization is a ubiquitous regulatory mechanism that defines the activatable pool of receptors, and thus, the ability of cells to respond to environmental stimuli. In recent years, the molecular mechanisms controlling the desensitization of
Michelle B Henesy +7 more
doaj +2 more sources
Homologous β-adrenergic desensitization in isolated rat hepatocytes [PDF]
Biochemical Journal, 1987 Hepatocytes from hypothyroid rats have a marked beta-adrenergic responsiveness. Preincubation of these hepatocytes with isoprenaline induced a time-dependent and concentration-dependent desensitization of the beta-adrenergic responsiveness without altering that to glucagon (homologous desensitization).
J. Adolfo García‐Sáinz +1 more
openalex +4 more sources
Modeling the Role of Homologous Receptor Desensitization in Cell Gradient Sensing [PDF]
The Journal of Immunology, 2008 Abstract G-protein-coupled chemoattractant receptors signal transiently upon ligand binding to effect cell orientation and motility but then are rapidly desensitized. The importance of desensitization has been unclear, because mutated nondesensitizable receptors mediate efficient chemotaxis.
Francis Lin, Eugene C. Butcher
openalex +4 more sources
Divergent Mechanisms for Homologous Desensitization of p21 by Insulin and Growth Factors [PDF]
Journal of Biological Chemistry, 1995 Previous work suggested that desensitization of p21ras in response to growth factors such as epidermal growth factor (EGF) results from receptor down-regulation. Here we show that p21ras is desensitized by insulin in 3T3-L1 adipocytes in the continued presence of activated insulin receptors, while loss of epidermal growth factor and platelet-derived ...
Jes K. Klarlund +2 more
openalex +5 more sources
μ‐Opioid receptor desensitization: homologous or heterologous? [PDF]
European Journal of Neuroscience, 2012 AbstractThere is considerable controversy over whether μ‐opioid receptor (MOPr) desensitization is homologous or heterologous and over the mechanisms underlying such desensitization. In different cell typesMOPr desensitization has been reported to involve receptor phosphorylation by various kinases, includingG‐protein‐coupled receptor kinases (GRKs ...
Javier Llorente +6 more
openalex +5 more sources
α1B-adrenergic receptors differentially associate with Rab proteins during homologous and heterologous desensitization. [PDF]
PLoS ONE, 2015 Internalization of G protein-coupled receptors can be triggered by agonists or by other stimuli. The process begins within seconds of cell activation and contributes to receptor desensitization.
Jean A Castillo-Badillo +5 more
doaj +3 more sources
Cellular Physiology and Biochemistry, 2013 Background/Aims: Signalling via CysLT1 is involved in activation of volume sensitive K+ channels and homologous desensitization of the LTD4 receptor impairs regulatory volume decrease (RVD). The aim is to illustrate the effect of mutation of putative PKC
Sune T. Jørgensen +5 more
doaj +2 more sources
TRAF6-mediated ubiquitination of AKT in the nucleus is a critical event underlying the desensitization of G protein-coupled receptors [PDF]
Cell Communication and SignalingBackground Desensitization of G protein–coupled receptors (GPCRs) refers to the attenuation of receptor responsiveness by prolonged or intermittent exposure to agonists.
Chengyan Wu +7 more
doaj +2 more sources