A NONIMMUNOSUPPRESSIVE TRIENE-MODIFIED RAPAMYCIN ANALOG IS A POTENT INHIBITOR OF PEPTIDYL-PROLYL CIS-TRANS ISOMERASE

被引：31

作者：

OCAIN, TD ^{[1
]}

LONGHI, D ^{[1
]}

STEFFAN, RJ ^{[1
]}

CACCESE, RG ^{[1
]}

SEHGAL, SN ^{[1
]}

机构：

[1] WYETH AYERST RES, PRINCETON, NJ 08543 USA

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1993年 / 192卷 / 03期

关键词：

D O I：

10.1006/bbrc.1993.1563

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A triene-modified analog of the potent immunosuppressive agent rapamycin was found to be a potent inhibitor of the peptidyl prolyl cis-trans isomerase activity of human FKBP (K(i) = 12.5 nM). This analog was not immunosuppressive in a thymocyte proliferation assay itself, but was able to antagonize the effect of rapamycin. This new analog should be useful as a mechanistic probe for macrocyclic immunosuppressants. © 1993 Academic Press, Inc.

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页码：1340 / 1346

页数：7

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