CONFORMATION OF 2 NONIMMUNOSUPPRESSIVE FK506 ANALOGS WHEN BOUND TO FKBP BY ISOTOPE-FILTERED NMR

被引：52

作者：

PETROS, AM ^{[1
]}

KAWAI, M ^{[1
]}

LULY, JR ^{[1
]}

FESIK, SW ^{[1
]}

机构：

[1] ABBOTT LABS,DIV PHARMACEUT DISCOVERY,D-47G AP9,ABBOTT PK,N CHICAGO,IL 60064

来源：

FEBS LETTERS | 1992年 / 308卷 / 03期

关键词：

FKBP; FK506; IMMUNOSUPPRESSANT; NMR;

D O I：

10.1016/0014-5793(92)81300-B

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：

The 3D structure of two unlabeled FK506 analogs, (R)- and (S)-[18-OH]ascomycin, when bound to [U-C-13,N-15]FKBP were determined by isotope-filtered 2D NMR experiments. The structures for the R and S isomers that bind tightly to FKBP but lack immunosuppressive activity are compared to each other and to the conformation of the potent immunosuppressant, ascomycin, when bound to FKBP. The results are interpreted in terms of calcineurin binding to the FKBP/ascomycin complex.

引用

页码：309 / 314

页数：6

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