Literature DB >> 15387654

BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp.

Olivier Potterat1, Klaus Wagner, Gerd Gemmecker, Jürgen Mack, Carsten Puder, Regine Vettermann, Rüdiger Streicher.   

Abstract

A new bicyclic 19-peptide, BI-32169, has been isolated from the culture broth of Streptomyces sp. (DSM 14996). Its structure has been established by amino acid analysis, mass spectrometry, and 2D NMR analysis. BI-32169 consists exclusively of protein amino acids and is cyclized from the side chain of Asp(9) to the N-terminus of Gly(1). One disulfide bond between Cys(6) and Cys(19) forms a bicyclic structure. BI-32169 and its methyl ester derivative showed potent inhibitory activity against the human glucagon receptor (IC(50) 440 and 320 nM, respectively) in a functional cell-based assay.

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Year:  2004        PMID： 15387654     DOI： 10.1021/np040093o

Source DB:  PubMed          Journal:  J Nat Prod        ISSN： 0163-3864            Impact factor:   4.050


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