Rediscovering an endothelin antagonist (BQ-123): A self-deconvoluting cyclic pentapeptide library

…, Y Crozet, D deWit, M Yanagisawa

Index: Spatola, Arno F.; Crozet, Yvon; DeWit, Damiane; Yanagisawa, Masashi Journal of Medicinal Chemistry, 1996 , vol. 39, # 19 p. 3842 - 3846

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Citation Number: 76

Abstract

A “self-deconvoluting” cyclic pentapeptide library, designed to produce 82 944 head-to-tail- linked peptides in 48 vials, has been prepared. The mixture included amino acids found in a recently optimized endothelin antagonist, BQ-123, originally isolated from microbial sources by Banyu investigators. Using a positional scan approach, the most potent of 12 residues at each of the four variable positions uniquely rediscovered the BQ-123 sequence or cyclo (l- ...