G Protein Coupled Bile Acid Receptor 1 gains Edge as Inflammation Controllers

Posted by Deeksha on October 7th, 2019

Gene G protein coupled bile acid receptor 1 (GPBAR1) is known to encode a member belonging to  superfamily G protein coupled receptor (GPCR) that acts as bile acid receptor on cell surface. Activation of MAP kinase signaling pathway, receptor internalization and production of intracellular cAMP is induced by treatment of cells that are involved in expression of the encoded GPCR. G coupled bile acid receptor 1 has emerged as a promising target that can be employed in treatment of various diseases such as type 2 diabetes, atherosclerosis, obesity and fatty liver disease. Researches and studies dedicated to identification of GPBAR1 agonists are of huge relevance for these diseases as the number of effected population has been increasing, creating demand for pharmaceutical and therapeutic solutions. The rising demand boosts G protein coupled bile acid receptor 1 market. An intelligence report titled, “G Protein Coupled Bile Acid Receptor 1-Pipeline Review, H2 2019” is the source of all the stated insights. This report is the latest addition to Market Research Hub’s ever growing repository.

In the quest of pharmacological therapeutic needs, a protocol was setup initiating collection of all structural information available about the ligand that was used in generation of ligand-based pharmacophore models in advanced LigandScout4.08. Pharmacophore model is 3D representation of interactions at molecular levels between legand structure and target which undergoes further reduction to chemical and steric features necessary to trigger a pharmacological effect.

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GPBAR1 is presumed significant for its contributions in glucose homeostasis and energy expenditure. Series of isonicotinamides exemplified by compound 3 that are identified as non-steroidal GPBAR1 agonists was optimized to potent derivatives that are known to be active on both  ? Murine GPBAR1 and humans. Secretion of pro-inflammatory cytokines IL-?? and TNF-? is inhibited by the GPBAR1 agonists whereas this impact of inhibition is absent on anti-inflammatory IL-10 present in primary human monocytes. Furthermore, these GPBAR1 agonists are actively involved in stabilization of phenotypes of non- inflammatory and alternative M2-like cells while the monocytes differentiate into macrophages. GBPAR1 agonists serve as inflammation controllers.

G protein coupled bile acid receptor 1: Report Synopsis

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G protein coupled bile acid receptor 1: Research Methodology

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