PMID: 9437737Jan 23, 1998Paper

Comparative study of in vitro and in vivo activities of bombesin pseudopeptide analogs modified on the C-terminal dipeptide fragment

Peptides
J AzayJ Martinez

Abstract

Analogs of bombesin in which the peptide bond between the two last amino acid residues were replaced by a pseudopeptide bond mimicking the transition state analog were evaluated. These compounds were able to recognize the bombesin receptor on isolated rat pancreatic acini with high potency (Ki from 0.60 +/- 0.27 nM to 4.3 +/- 2.3 nM). Although they were devoid of agonist activity, they were able to antagonize bombesin-induced amylase secretion in this model, with potencies in accordance with their affinities (IC50 from 1.6 +/- 0.3 nM to 10.0 +/- 1.7 nM). When tested in vivo in the anesthetized rat, these bombesin receptor antagonists exhibited high potency in inhibiting bombesin-induced pancreatic secretion (H-DPhe-Gln-Trp-Ala-Val-Gly-His-NH-CH[CH2-CH(CH3)2]-CHOH-(CH 2)3-CH3, JMV845, was among the most potent compounds with ED50 of 7.82 +/- 2.89 nM in inhibiting bombesin-induced protein secretion). The results of this study showed that replacing the peptide bond between the two last amino acid residues in bombesin by mimicking the transition state analog resulted in in vitro and in vivo potent bombesin receptor antagonists.

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Citations

Aug 19, 2010·European Journal of Nuclear Medicine and Molecular Imaging·Rosalba MansiHelmut R Maecke
Oct 7, 2014·Cancer Biotherapy & Radiopharmaceuticals·Panteleimon J MarsouvanidisMarion de Jong
Jul 27, 2007·European Journal of Pharmacology·Hong WuDaling Zhu
Apr 25, 2020·Bioorganic Chemistry·Fariba MalekiNourollah Sadeghzadeh
Nov 15, 2011·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Keelara AbirajHelmut R Maecke
Jul 12, 2016·Bioconjugate Chemistry·Yao SunXuechuan Hong

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