Orphan GPCR research

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An orphan GPCR finds a home in the heart.

G PROTEIN-COUPLED RECEPTORS (GPCRs) are the largest and most successful targets for pharmacotherapy to date, particularly in the area of cardiovascular disease. These receptors are at the forefront of current drug discovery efforts (7). GPCRs also form the largest family of transmembrane receptors, with nearly 800 GPCR loci (12, 18), of which several hundred are categorized as orphan GPCRs. The...

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Development of new in silico methods to identify ligands for orphan GPCR

In the first step of our procedure, ligand-based, as well as receptor-based fingerprints are constructed. The receptorfingerprints are based on the physico-chemical properties of residues lining the transmembrane cavities of GPCR homology models [1,2]. The ligand-fingerprints are derived from Shannon Entropy of pairwise distributions of atom properties. In a second step, the two fingerprints ar...

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The Orphan Adhesion-GPCR GPR126 Is Required for Embryonic Development in the Mouse

Adhesion-GPCRs provide essential cell-cell and cell-matrix interactions in development, and have been implicated in inherited human diseases like Usher Syndrome and bilateral frontoparietal polymicrogyria. They are the second largest subfamily of seven-transmembrane spanning proteins in vertebrates, but the function of most of these receptors is still not understood. The orphan Adhesion-GPCR GP...

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ژورنال

عنوان ژورنال: British Journal of Pharmacology

سال: 2008

ISSN: 0007-1188

DOI: 10.1038/sj.bjp.0707606