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一种来自包含苄基取代氮杂双环烷氨基酸的环状RGD五肽模拟物小文库的强效整合素拮抗剂。

A potent integrin antagonist from a small library of cyclic RGD pentapeptide mimics including benzyl-substituted azabicycloalkane amino acids.

作者信息

Arosio Daniela, Belvisi Laura, Colombo Lino, Colombo Matteo, Invernizzi Donatella, Manzoni Leonardo, Potenza Donatella, Serra Massimo, Castorina Massimo, Pisano Claudio, Scolastico Carlo

机构信息

Istituto di Scienze e Tecnologie Molecolari, Consiglio Nazionale delle Ricerche, Via Fantoli 16/15, 20138 Milano, Italy.

出版信息

ChemMedChem. 2008 Oct;3(10):1589-603. doi: 10.1002/cmdc.200800143.

DOI:10.1002/cmdc.200800143
PMID:18770516
Abstract

A small library of cyclic RGD pentapeptide mimics, including benzyl-substituted azabicycloalkane amino acids, was synthesized with the aim of developing active and selective integrin antagonists. In vitro binding assays established one particular compound with affinity for both the alpha(v)beta(3) and the alpha(v)beta(5) integrins. The synthesis in solution and the in vitro screening of these RGD derivatives, as well as the determination of the conformational properties of the integrin ligands by spectroscopic and computational methods are described.

摘要

合成了一个包含苄基取代氮杂双环烷氨基酸的环状RGD五肽模拟物小型文库，目的是开发活性和选择性整合素拮抗剂。体外结合试验确定了一种对α(v)β(3)和α(v)β(5)整合素均具有亲和力的特定化合物。描述了这些RGD衍生物的溶液合成、体外筛选以及通过光谱和计算方法测定整合素配体的构象性质。

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