ATOMIC-STRUCTURE OF FKBP-FK506, AN IMMUNOPHILIN-IMMUNOSUPPRESSANT COMPLEX

被引：628

作者：

VANDUYNE, GD

STANDAERT, RF

KARPLUS, PA

SCHREIBER, SL

CLARDY, J

机构：

[1] HARVARD UNIV,DEPT CHEM,CAMBRIDGE,MA 02138

[2] CORNELL UNIV,DEPT BIOCHEM MOLEC & CELL BIOL,ITHACA,NY 14853

[3] CORNELL UNIV,DEPT CHEM,BAKER LAB,ITHACA,NY 14853

来源：

SCIENCE | 1991年 / 252卷 / 5007期

关键词：

D O I：

10.1126/science.1709302

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

The structure of the human FK506 binding protein (FKBP), complexed with the immunosuppressant FK506, has been determined to 1.7 angstroms resolution by x-ray crystallography. The conformation of the protein changes little upon complexation, but the conformation of FK506 is markedly different in the bound and unbound forms. The drug's association with the protein involves five hydrogen bonds, a hydrophobic binding pocket lined with conserved aromatic residues, and an unusual carbonyl binding pocket. The nature of this complex has implications for the mechanism of rotamase catalysis and for the biological actions of FK506 and rapamycin.

引用

页码：839 / 842

页数：4

共 23 条

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