X-linked form of Kallmann syndrome (KS), characterized by hypogonadotropic hypogonadism and anosmia, is due We also show that the N-terminal region of anosmin 1, capable of binding to the PK2-binding domain of The whey acidic protein domain (WAP) is necessary for this modulatory activity, although data from GST domain 1 (FnIII.1) suggest the cysteine-rich (CR) and the FnIII.1 domains could assist the WAP domain Read more at the source #DrGPCR #GPCR #IndustryNews

2022 Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic diabetes insipidus "Loss-of-function mutations of the arginine vasopressin receptor 2 gene (AVPR2) cause Nephrogenic diabetes relationship between the conformational change of the receptor because of the mutation and related downstream Their functionality in terms of cAMP production via Gαs protein coupling was decreased compared to the Read more at the source #DrGPCR #GPCR #IndustryNews

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of the transcriptional coactivator β-catenin by recruiting the cytosolic effector Dishevelled (Dvl). Polymerization of Dvl at the plasma membrane recruits the β-catenin destruction complex, enabling the Moreover, binding to Fzd did not promote Dvl DEP domain dimerization, which has been proposed to be required for signaling downstream of Fzd. Read more at the source #DrGPCR #GPCR #IndustryNews

2022 " Background and purpose: The interaction of arrestins with G-protein coupled receptors (GPCRs) desensitizes agonist-dependent receptor responses and often leads to receptor internalization. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin Interestingly, both cell lines displayed different complements of β-arrestin 1 and 2 expression. or pro-metastatic behaviour, as divergent responses were observed in the two TNBC lines tested. Whether this divergence is related to the observed differences in β-arrestin complements warrants further Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Epithelium That Directs P-Glycoprotein Expression "P-glycoprotein (P-gp) is a key component of the intestinal We now aim to determine the molecular mechanism by which this functional microbiome output regulates These findings shed light on a sophisticated signaling network directed by intestinal microbial metabolites Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent the expression of plasminogen activator inhibitor type<br />1 (PAI-1) which leads to cardiovascular disorders The purpose of this study was to evaluate the role of dual transactivation of EGF and TGF-β receptors of G protein-coupled receptor (GPCR) signaling, the functions of ROCK and PLC were investigated in dual Read more at the source #DrGPCR #GPCR #IndustryNews

activation of phospholipase C (PLC) is thought to have a key role in the cardiomyocyte response to several different PLC activity results in the generation of diacylglycerol and inositol trisphosphate, which are downstream In this article, we describe the signal transduction elements that regulate PLC gene expression. The discussion is focused on the norepinephrine- α1-adrenoceptor signaling pathway and downstream signaling Read more at the source #DrGPCR #GPCR #IndustryNews

Multiple 14-3-3 isoforms exist, and a GPCR can differentially interact with different 14-3-3 isoforms adaptor complexes during endocytosis. a degradation process. development by modulating GPCR/14-3-3 signals temporally." Read more at the source #DrGPCR #GPCR #IndustryNews

Due to increasing numbers of people with excess body weight, the MC4R has become a target of interest NanoBRETTM studies to determine protein–protein interaction were conducted, confirming decreased homodimerization Results demonstrate an improvement of alpha-MSH-induced NFAT signaling of chimeras, reaching the level Read more at the source #DrGPCR #GPCR #IndustryNews

of membrane constituents into domains. Our results show that the short-term diffusion coefficient of the receptor decreases upon cholesterol depletion, irrespective of the method of cholesterol depletion. change upon cholesterol depletion. accompanied by a reduction in diffusion coefficient for chronic cholesterol depletion.

domains linked to transmembrane heptahelical (HH) bundles. of calcium metabolism are not yet clearly defined. When the same mutation was present in both VFT domains of receptor dimers, analogous to homozygous neonatal Thus two WT VFT domains were required for normal Ca2+o potency and there was a pronounced gene-dosage Read more at the source #DrGPCR #GPCR #IndustryNews

We are able to identify the interaction of membrane cholesterols with definite sites and domains within domain (CRD) and the intracellular domain (ICD), are through residues belonging to known cholesterol-binding Structural analysis of SMO domains shows significant changes in the CRD and ICD, during the course of Further detailed analysis of the dynamics of the TMD reveals the movements of TM5, TM6, and TM7, linked Read more at the source #DrGPCR #GPCR #IndustryNews

under cholesterol-depleted condition. For this, we analyzed the lateral dynamics of the serotonin1A receptor in cholesterol-depleted cells with models describing the diffusion of molecules in a homogeneous membrane. Interestingly, these parameters are altered in cholesterol-depleted cells and the receptor exhibits dynamic Notably, our results show that statin-induced dynamic confinement could be reversed by destabilization

September 2022 Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin Signaling Axis by Repurposing Vaptans "Men with advanced prostate cancer are treated by androgen deprivation therapy but the disease recurs as incurable castration-resistant prostate cancer (CRPC), requiring new highly correlated with disease progression. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify receptor-transducer receptor (GPCR) GPR35 is involved in oncogenic signaling, bacterial infections, and inflammatory bowel disease GPR35 is known to be expressed as two distinct isoforms that differ only in the length of their extracellular N-termini by 31 amino acids, but detailed insights into their functional differences are lacking. Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 GASP1 enhances malignant phenotypes of breast cancer cells and decreases their response Here, we demonstrated that GASP1 was highly expressed in breast cancers, and patients harboring altered ) by competitively binding to IGF1R with ubiquitin E3 ligase MDM2, thereby activating its downstream Collectively, this study demonstrates that GASP1 enhances malignant behaviors of breast cancer cells Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent The multiple downstream signaling pathways are still poorly understood. Here, we focused on disclosing the integrin-dependent roles of focal adhesion kinase (protein tyrosine Together, these data reveal a shear-dependent signaling axis of PTK2, integrin αIIbβ3, and CIB1 in collagen Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization The spatial pattern of GPCR phosphorylation is predicted to trigger these discrete GRK and arrestin-mediated Here, we provide evidence that distal carboxyl-terminal tail (C-tail), but not proximal, phosphorylation of the chemokine receptor CXCR4 specifies βarrestin1 (βarr1)-dependent signaling. Read more at the source #DrGPCR #GPCR #IndustryNews

Disruption of normal glutamate transmission has been implicated in a variety of neurodegenerative and neuropsychiatric diseases. sclerosis, Alzheimer's disease, Huntington's disease, Parkinson's diseases, schizophrenia and depression as well as drug addiction. Read more at the source #DrGPCR #GPCR #IndustryNews