A STRUCTURAL ROLE FOR HORMONE IN THE THYROID-HORMONE RECEPTOR

被引：781
作者：
WAGNER, RL
APRILETTI, JW
MCGRATH, ME
WEST, BL
BAXTER, JD
FLETTERICK, RJ
机构：
[1] UNIV CALIF SAN FRANCISCO, METAB RES UNIT, SAN FRANCISCO, CA 94143 USA
[2] UNIV CALIF SAN FRANCISCO, DEPT MED, SAN FRANCISCO, CA 94143 USA
[3] UNIV CALIF SAN FRANCISCO, DEPT BIOCHEM & BIOPHYS, SAN FRANCISCO, CA 94143 USA
[4] KHEPRI PHARMACEUT INC, San Francisco, CA 94080 USA
来源：
NATURE | 1995年 / 378卷 / 6558期
关键词：
D O I：
10.1038/378690a0
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 crystal structure of the rat a, thyroid hormone receptor ligand-binding domain bound with a thyroid hormone agonist reveals that ligand is completely buried within the domain as part of the hydrophobic core. In addition, the carboxy-terminal activation domain forms an amphipathic helix, with its hydrophobic face constituting part of the hormone binding cavity. These observations suggest a structural role for ligand, in establishing the active conformation of the receptor, that is likely to underlie hormonal regulation of gene expression for the nuclear receptors.
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页码：690 / 697
页数：8
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