November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

GPCRs represent major drug targets, as indicated by the fact that about 40% of all drugs currently used in clinical practice mediate their therapeutic effects by acting on GPCRs. Like many other organs, various GPCRs play a role in regulating liver function. It is predicted that more than 50 GPCRs are expressed in the liver. However, our knowledge of how GPCRs regulate liver metabolism and fibrosis in the different cell types

protein-coupled receptor expression: Implications for metabolic regulation G protein-coupled receptors (GPCRs their secretion of insulin, and islet function can be modified by ligands acting at the large number of GPCRs and, in this review, we have compared expression of GPCR mRNAs in human islets obtained from normal We have also considered the likely outcomes on islet function that the altered GPCR expression status confers and the possible impact that adipokines, secreted from expanded fat depots, could have at those GPCRs

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In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while In this way, we present the analysis of a series of GPCRs whose activity has been shown to affect the Our compilation of data revealed that the mechanisms most involved in the role of GPCRs in lifespan are possibility of using agonist or antagonist drugs, depending on the beneficial or harmful effects of each GPCR

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Lysophosphatidic acids (LPAs) are bioactive phospholipids implicated in a wide range of cellular activities that regulate a diverse array of biological functions. They recognize two types of G protein-coupled receptors (LPARs): LPA1-3 receptors and LPA4-6 receptors that belong to the endothelial gene (EDG) family and non-endothelial gene family, respectively. In recent years, the LPA signaling pathway has captured an increasing amount of attention because of its involvement in various diseases, such as idiopathic pulmonary fibrosis, cancers, cardiovascular diseases and neuropathic pain, making it a promising target for drug development. While no drugs targeting LPARs have been approved by the FDA thus far, at least three antagonists have entered phase Ⅱ clinical trials for idiopathic pulmonary fibrosis (BMS-986020 and BMS-986278) and systemic sclerosis (SAR100842), and one radioligand (BMT-136088/18F-BMS-986327) has entered phase Ⅰ clinical trials for positron emission tomography (PET) imaging of idiopathic pulmonary fibrosis. This article provides an extensive review on the current status of ligand development targeting LPA receptors to modulate LPA signaling and their therapeutic potential in various diseases. Read full article

vitro and in vivo data suggest that GHSR1a heterodimerises with multiple G protein-coupled receptors (GPCRs This review discusses the signalling mechanisms of GHSR1a alone and in combination with other GPCRs, and explores the physiological consequences of GHSR1a coupling with other GPCRs.

Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs Using current knowledge on class A GPCRs and existing experimental data in the literature as constraints

We also identified two Gs-coupled GPCRs that are endogenously expressed by SKM at relatively high levels

mechanosensation-dependent behavior in C. elegans via a trans function Latrophilins are highly conserved Adhesion GPCRs

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of the Inflammatory Cytokine IL-6 and Is Dependent on NF-κB Signaling G protein-coupled receptors (GPCRs Members of the Mas-related G protein coupled receptors (MRGPRs), a subfamily of GPCRs, are largely expressed

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positions in class A G protein-coupled receptors expressed in tumors G protein-coupled receptors (GPCRs Because there are many more GPCRs than effectors, mutations in different receptors could perturb signaling may not be enriched within a single gene but rather that cognate mutations with similar effects on GPCR To test this possibility, we systematically aggregated somatic cancer mutations across class A GPCRs The possibility that multiple different GPCRs could moonlight as drivers or enablers of a given cancer

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receptor-ligand complexes: Impact of ligand type and receptor activation state G protein-coupled receptors (GPCR Their abundance and role in nearly all physiological systems make GPCR the largest protein family targeted provided broadly generalizable performance expectations for docking into experimentally-characterized GPCR Simulations were performed using 37 experimental structures of 11 Class A GPCR crystallized in multiple Therefore, docking performance against GPCR targets can be estimated in advance based on docking target

G protein-coupled receptors (GPCRs) are integral to cellular signaling, influencing a wide array of physiological advancements in transcriptomic profiling have provided new insights into the expression patterns of GPCRs The study reports that human white blood cells express an average of 160 GPCR mRNAs, ranging from 123 to 206, while platelets exhibit a distinct profile with 69 GPCR mRNAs. abundant and rare GPCR transcripts.

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Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of the chemokine receptor CXCR4 WHIM syndrome is a rare immunodeficiency disorder that is characterized by warts, hypogammaglobulinemia, infections, and myelokathexis. While several gain-of-function mutations that lead to C-terminal truncations, frame shifts and point mutations in the chemokine receptor CXCR4 have been identified in WHIM syndrome patients, the functional effect of these mutations are not fully understood. Here, we report on a new WHIM syndrome mutation that results in a frame shift within the codon for Ser339 (S339fs5) and compare the properties of S339fs5 with wild type CXCR4 and a previously identified WHIM syndrome mutant, R334X. The S339fs5 and R334X mutants exhibited significantly increased signaling compared to wild type CXCR4 including agonist-promoted calcium flux and extracellular signal-regulated kinase activation. This increase is at least partially due to a significant decrease in agonist-promoted phosphorylation, β-arrestin binding, and endocytosis of S339fs5 and R334X compared to wild type CXCR4. Interestingly, there were also significant differences in receptor degradation, with S339fs5 having a very high basal level of degradation compared to that of R334X and wild type CXCR4. In contrast to wild type CXCR4, both R334X and S339fs5 were largely insensitive to CXCL12-promoted degradation. Moreover, while basal and agonist-promoted degradation of wild type CXCR4 was effectively inhibited by the CXCR4 antagonist TE-14016, this had no effect on the degradation of the WHIM mutants. Taken together, these studies identify a new WHIM syndrome mutant, CXCR4-S339fs5, that promotes enhanced signaling, reduced phosphorylation, β-arrestin binding and endocytosis, and a very high basal rate of degradation that is not protected by antagonist treatment. Read full article

Ahoy, GPCR Crew! GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Classified GPCR News  Let’s dive into the   Classified GPCR News from September 16th to 22nd, 2024 Industry Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug

Neuropeptides and their specific receptors (primarily G protein-coupled receptors, GPCRs) regulate multiple A total of 41 neuropeptide GPCR genes belonging to three classes were also identified. These GPCRs and their probable ligands were predicted. expression patterns of these 98 genes in various larval tissues were evaluated using quantitative real-time PCR to determine physiological functions and pharmacological characterization of neuropeptides and their GPCRs

Significant advancements in the cellular biology of G protein-coupled receptors (GPCRs) about a novel fluorescence serves as a readout for the activity of APEX2 and, by extension, the trafficking of the GPCR The development of molecular tools to study GPCR trafficking in real-time opens new avenues for understanding The implications of this research extend beyond basic science ; understanding the role of DNAJC13 in GPCR field continues to evolve, this study represents a crucial step toward unraveling the understanding of GPCR

GPCR ecosystem members!  GPCR ecosystem.  Top candidates will have a solid foundation in GPCR pharmacology as well as some experience in drug discovery GPCR