Discovery of galectin ligands in fully randomized combinatorial one-bead-one-compound (glyco)peptide libraries

被引：62

作者：

Andre, Sabine

Maljaars, C. Elizabeth P.

Halkes, Koen M.

Gabius, Hans-Joachim

Kamerling, Johannis P.

机构：

[1] Univ Utrecht, Dept Bioorgan Chem, Bijvoet Ctr, NL-3584 CH Utrecht, Netherlands

[2] Univ Munich, Fac Med Vet, Inst Physiol Chem, D-80539 Munich, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 03期

关键词：

combinatorial (glyco)peptide libraries; galectins;

D O I：

10.1016/j.bmcl.2006.10.067

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The involvement of human lectins (galectins) in disease progression accounts for the interest to design potent inhibitors. Three fully randomized hexa(glyco)peptide libraries were prepared using the portion mixing method combined with ladder synthesis. On-bead screening with fluorescently labelled galectin-1 and -3 yielded a series of lead structures, whose inhibitory activity on carbohydrate-dependent galectin binding was tested in solution by solid-phase and cell assays. The various data obtained define the library approach as a facile route for the discovery of selective (glyco)peptide-based galectin inhibitors. (c) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：793 / 798

页数：6

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