1A28

HORMONE-BOUND HUMAN PROGESTERONE RECEPTOR LIGAND-BINDING DOMAIN

1A28 の概要

• エントリーDOI: 10.2210/pdb1a28/pdb
• 分子名称: PROGESTERONE RECEPTOR, PROGESTERONE (3 entities in total)
• 機能のキーワード: progesterone receptor, steroid receptor, nuclear receptor, transcription regulation
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Nucleus. Isoform A: Nucleus: P06401
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 59738.19

構造登録者

Sigler, P.B.,Williams, S.P. (登録日: 1998-01-19, 公開日: 1998-07-15, 最終更新日: 2024-02-07)

主引用文献

Williams, S.P.,Sigler, P.B.
Atomic structure of progesterone complexed with its receptor.
Nature, 393:392-396, 1998

PubMed Abstract: The physiological effects of progestins are mediated by the progesterone receptor, a member of the steroid/nuclear receptor superfamily. As progesterone is required for maintenance of pregnancy, its receptor has been a target for pharmaceuticals. Here we report the 1.8 A crystal structure of a progesterone-bound ligand-binding domain of the human progesterone receptor. The nature of this structure explains the receptor's selective affinity for progestins and establishes a common mode of recognition of 3-oxy steroids by the cognate receptors. Although the overall fold of the progesterone receptor is similar to that found in related receptors, the progesterone receptor has a quite different mode of dimerization. A hormone-induced stabilization of the carboxy-terminal secondary structure of the ligand-binding domain of the progesterone receptor accounts for the stereochemistry of this distinctive dimer, explains the receptor's characteristic pattern of ligand-dependent protease resistance and its loss of repression, and indicates how the anti-progestin RU486 might work in birth control. The structure also indicates that the analogous 3-keto-steroid receptors may have a similar mechanism of action.

PubMed: 9620806
DOI: 10.1038/30775

実験手法

X-RAY DIFFRACTION (1.8 Å)