BI-32169，一种来自链霉菌属的具有强胰高血糖素受体拮抗剂活性的双环19肽。
BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp.
作者信息
Potterat Olivier, Wagner Klaus, Gemmecker Gerd, Mack Jürgen, Puder Carsten, Vettermann Regine, Streicher Rüdiger
机构信息
Boehringer Ingelheim Pharma GmbH and Co. KG, Birkendorfer Strasse 65, D-88397 Biberach an der Riss, Germany.
出版信息
J Nat Prod. 2004 Sep;67(9):1528-31. doi: 10.1021/np040093o.
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.
一种新的双环19肽BI-32169已从链霉菌属（DSM 14996）的培养液中分离出来。其结构已通过氨基酸分析、质谱和二维核磁共振分析得以确定。BI-32169仅由蛋白质氨基酸组成，并且从Asp(9)的侧链环化至Gly(1)的N端。Cys(6)和Cys(19)之间的一个二硫键形成双环结构。在基于细胞功能的检测中，BI-32169及其甲酯衍生物对人胰高血糖素受体显示出强效抑制活性（IC(50)分别为440和320 nM）。
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