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Binding of progastrin fragments to the 78 kDa gastrin‐binding protein
Author(s) -
Baldwin Graham S.
Publication year - 1995
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(95)00017-4
Subject(s) - gastrin , proglumide , autocrine signalling , receptor , chemistry , cholecystokinin , gastrointestinal hormone , cholecystokinin receptor , biochemistry , peptide hormone , medicine , endocrinology , secretion , biology
The non‐selective gastrin/cholecystokinin receptor antagonists proglumide and benzotript inhibit colon carcinoma cell proliferation by binding to the 78 kDa gastrin‐binding protein (GBP) (Baldwin, Proc. Natl. Acad. Sci. USA, 91 (1994) 7593–7597). However, although most colon carcinoma cell lines synthesize progastrin, production of mature amidated gastrin 17 has not been observed. In order to define the structural requirements for the binding of gastrin to the GBP the affinities of various fragments of amidated and C‐terminally extended gastrin 17 for the GBP have been measured. The results indicate that the GBP recognizes both N‐ and C‐termini of gastrin 17 . Moreover since C‐terminal amidation is not a prerequisite for binding of gastrin to the GBP, the GBP is a potential target for the autocrine effects of progastrin.