A STRUCTURAL ROLE FOR HORMONE IN THE THYROID-HORMONE RECEPTOR

被引：778

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.

引用

页码：690 / 697

页数：8

共 49 条

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