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• W1567236738 startingPage "11258" @default.
• W1567236738 abstract "Abstract Gastrin releasing peptide (GRP) is a 27-residue peptide hormone which is analogous to the amphibian peptide bombesin. GRP serves a variety of physiological functions and has been implicated as an autocrine factor in the growth regulation of small cell lung cancer cells. We have developed a series of potent GRP antagonists by modification of the COOH terminus of N-acetyl-GRP-20-27. The most potent member of this series, N-acetyl-GRP-20-26-OCH2CH3, exhibits an IC50 of 4 nM in a competitive binding inhibition assay. This compound blocks GRP-stimulated mitogenesis in Swiss 3T3 mouse fibroblasts, inhibits GRP-dependent release of gastrin in vitro, and blocks GRP-induced elevation of [Ca2+]i in H345 small cell lung cancer cells. These results demonstrate that while residues 20-27 of GRP influence binding of the parent peptide to its receptor, the COOH-terminal amino acid is primarily responsible for triggering the subsequent biological response." @default.
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• W1567236738 date "1989-07-01" @default.
• W1567236738 modified "2023-10-06" @default.
• W1567236738 title "Carboxyl-terminal Modification of a Gastrin Releasing Peptide Derivative Generates Potent Antagonists" @default.
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• W1567236738 doi "https://doi.org/10.1016/s0021-9258(18)60457-0" @default.
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