Transglutaminase surface recognition by peptidocalix[4]arene diversomers

被引：42

作者：

Francese, S

Cozzolino, A

Caputo, L

Esposito, C

Martino, M

Gaeta, C

Troisi, F

Neri, P

机构：

[1] Univ Salerno, Dipartimento Chim, I-84081 Baronissi, Salerno, Italy

[2] Univ Naples Federico II, Dipartimento Pediat, I-80131 Naples, Italy

[3] Univ Naples Federico II, Dipartimento Sci Alimenti, I-80055 Naples, Italy

来源：

TETRAHEDRON LETTERS | 2005年 / 46卷 / 10期

关键词：

calixarenes; peptidocalixarenes; transglutaminase; surface protein recognition; enzyme inhibitors;

D O I：

10.1016/j.tetlet.2005.01.078

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of N-linked tetrakis(tetrapeptido)calix[4]arene diversomers, 3A-P, has been synthesized by Coupling of a cone calix[4]arene tetracarboxylic acid chloride with tetrapeptides 1A-P obtained in a parallel fashion. The inhibition activity of 3A-P towards tissue and microbial transglutaminase was evaluated by in vitro assays with a labeled substrate. Kinetic analysis using one of the most active derivatives (3A) showed a noncompetitive inhibition with respect to the amino acceptor Substrate and an uncompetitive inhibition with respect to amino donor substrate. Experimental results are in accordance with ail inhibition due to a protein specific surface recognition on a region noncomprising the enzyme active site. (C) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1611 / 1615

页数：5