Gastrin-Releasing Peptide Receptor (GRPR)
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The human gastrin-releasing peptide receptor (hGRPR) gene was cloned in 1990 from NIH3T3 cells and located on chromosome X (Xp22.2–Xp22.13). It encodes a seven-transmembrane α-helices G protein-coupled receptor (GPCR) of 384-aa, interacting with large heterotrimeric G proteins of the Gαq and Gα12/ Gα13 families. The main GRPR ligands are represented by bombesin-like peptides (BLPs), including gastrin-releasing peptide (GRP) that is a peptide originally isolated from porcine stomach, synthesized as a precursor of 148-aa (PreproGRP) and post-translationally modified as a mature 27-aa neuropeptide. GRP is the mammalian homolog of the amphibian 14-aa peptide bombesin (BBS), sharing the same C-terminal sequence and binding to the same receptor. Four BLP binding receptor subtypes have been isolated: receptor subtype 1, termed GRPR, which binds BBS and GRP with high affinity; receptor subtype 2 binding neuromedin...
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