GPBAR1

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GPBAR1

A gene on chromosome 2q35 that encodes a G protein-coupled receptor for bile acid. Bile acid binding induces GPBAR1 internalisation, activation of extracellular signal-regulated kinase and intracellular cAMP production; it is believed to be involved in the suppression of macrophage functions by bile acids.
References in periodicals archive ?
This alliance with AstraZeneca illustrates the broad power and scalability of the Heptares technology to generate novel drug candidates in regions of GPCR space that were previously regarded as closed to pharmaceutical discovery," said Malcolm Weir, CEO of Heptares.
This publication represents the first account of an in vivo active pepducin agonist and demonstrates the promise for pepducin technology as a novel approach to target therapeutically important GPCRs.
Gave notice to Patobios Limited (Patobios) of Omeros' intent to acquire intellectual property assets from Patobios for use in our GPCR program.
In the current study, Jarvik and colleagues engineered a fluoromodule that would readily determine when GPCR retreats from the cell membrane.
PerkinElmer's current GPCR portfolio contains assay tool kits AlphaScreen ERK, LANCE and LANCE Ultra, which have broad potential for identifying cellular targets in a wide range of disease states including, hypertension, gastro-intestinal, and neurological disorders.
GPCRs are a family of proteins that are major, important screening targets in the drug discovery field.
The results are interpreted by LifeSpan's in-house pathologists and used to construct a relational database, which will contain detailed information on GPCR expression in each cell type in the tissues and diseases studied, accompanied by high resolution digital images.
Trevena's expertise lies in engineering "biased ligands" that activate only the beneficial signaling pathways downstream of a GPCR to unlock new biology and avoid drug adverse effects.
Omeros also has a proprietary G protein-coupled receptor (GPCR) platform, which is making an unprecedented number of new GPCR drug targets and corresponding compounds available to the pharmaceutical industry for drug development, as well as a platform used to generate antibodies.
Although one G protein GPCR complex has been crystallised this was exceedingly diffciult and resulted in poor resolution of the GPCR component of the complex.
Under this collaboration, Heptares will use its proprietary GPCR structure-guided platform to help deliver stabilised GPCRs (StaR proteins), high-resolution crystal structures and other technologies to support the discovery of potential novel agents directed to the GPCR targets selected by Pfizer.
describe the successful application of fragment screening to multiple GPCR targets that were stabilised, for the first time, using the Heptares StaR(r) technology.