Encyclopedia of Signaling Molecules

2018 Edition
| Editors: Sangdun Choi

Gastrin-Releasing Peptide Receptor (GRPR)

  • Alessia Parascandolo
  • Maria Domenica Castellone
Reference work entry
First Online:
DOI: https://doi.org/10.1007/978-3-319-67199-4_101646
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Synonyms

 BB2R;  GRPR;  GRP-preferring bombesin receptor

Historical Background

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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Copyright information

© Springer International Publishing AG 2018

Authors and Affiliations

  • Alessia Parascandolo
    • 1
  • Maria Domenica Castellone
    • 2
  1. 1.IRCCS SDNNaplesItaly
  2. 2.Institute of Experimental Endocrinology and Oncology (IEOS)CNRNaplesItaly