作为凝集素结合配体来源的新糖肽树枝状聚合物文库。

Neoglycopeptide dendrimer libraries as a source of lectin binding ligands.

作者信息

Kolomiets Elena, Johansson Emma M V, Renaudet Olivier, Darbre Tamis, Reymond Jean-Louis

机构信息

Department of Chemistry and Biochemistry, University of Berne, Freiestrasse 3, CH-3012, Berne, Switzerland.

出版信息

Org Lett. 2007 Apr 12;9(8):1465-8. doi: 10.1021/ol070119d. Epub 2007 Mar 13.

DOI:10.1021/ol070119d

PMID:17352485

Abstract

[structure: see text] A 15 625-membered peptide dendrimer combinatorial library was acylated with an alpha-C-fucosyl residue at its four N-termini and screened for binding to fucose-specific lectins. Dendrimer FD2 (Fuc-alpha-CH2CO-Lys-Pro-Leu)4(Lys-Phe-Lys-Ile)2Lys-His-Ile-NH2 was identified as a potent ligand against Ulex europaeus lectin UEA-I (IC50 = 11 microM) and Pseudomonas aeruginosa lectin PA-IIL (IC50 = 0.14 microM).

摘要

[结构：见正文] 一个由15625个成员组成的肽树枝状聚合物组合文库在其四个N端用α-C-岩藻糖基残基进行酰化，并筛选其与岩藻糖特异性凝集素的结合情况。树枝状聚合物FD2（Fuc-α-CH2CO-Lys-Pro-Leu）4（Lys-Phe-Lys-Ile）2Lys-His-Ile-NH2被鉴定为针对欧洲荆豆凝集素UEA-I（IC50 = 11微摩尔）和铜绿假单胞菌凝集素PA-IIL（IC50 = 0.14微摩尔）的有效配体。