SELECTIVE-INHIBITION OF TRYPANOSOMAL TRIOSEPHOSPHATE ISOMERASE BY A THIOPEPTIDE

被引：31

作者：

KESSLER, H

MATTER, H

GEYER, A

DIEHL, HJ

KOCK, M

KURZ, G

OPPERDOES, FR

CALLENS, M

WIERENGA, RK

机构：

[1] INT INST CELLULAR & MOLEC PATHOL,B-1200 BRUSSELS,BELGIUM

[2] EUROPEAN MOLEC BIOL LAB,W-6900 HEIDELBERG,GERMANY

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION IN ENGLISH | 1992年 / 31卷 / 03期

关键词：

D O I：

10.1002/anie.199203281

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

One approach to conquering sleeping sickness is the selective inhibition of trypanosomal triosephosphate isomerase, a key enzyme in the pathogen's metabolism, with cyclic hexapeptides. The thionylation of the Phe5-Phe6 amide bond of the cyclic hexapeptide cyclo(Gly1-Pro2-Phe3-Val4-Phe5-Phe6) is a minor modification, but effects a total rearrangement of the intramolecular hydrogen bonds which causes a drastic improvement of inhibitoric activity-maximum effect from minimum chemistry!

引用

页码：328 / 330

页数：3

共 21 条

[1] ARG-GLY-ASP CONSTRAINED WITHIN CYCLIC PENTAPEPTIDES - STRONG AND SELECTIVE INHIBITORS OF CELL-ADHESION TO VITRONECTIN AND LAMININ FRAGMENT-P1 [J].