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

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

  • J Nat Prod. 2004 Sep;67(9):1528-31. doi: 10.1021/np040093o.
Olivier Potterat 1,  Klaus Wagner,  Gerd Gemmecker,  Jürgen Mack,  Carsten Puder,  Regine Vettermann,  Rüdiger Streicher
Affiliations

Affiliation

  • 1 Boehringer Ingelheim Pharma GmbH and Co. KG, Birkendorfer Strasse 65, D-88397 Biberach an der Riss, Germany. olivier.potterat@bc.boehringer-ingelheim.com
PMID: 15387654 DOI: 10.1021/np040093o
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.

Figures