3ZRB

Structural basis for agonism and antagonism for a set of chemically related progesterone receptor modulators

3ZRB の概要

• エントリーDOI: 10.2210/pdb3zrb/pdb
• 関連するPDBエントリー: 1A28 1E3K 1SQN 1SR7 1ZUC 2C7A 2W8Y 3ZR7 3ZRA
• 分子名称: PROGESTERONE RECEPTOR, 2-CHLORO-N-[[4-(3,5-DIMETHYLISOXAZOL-4-YL)PHENYL]METHYL]-1,4-DIMETHYL-1H-PYRAZOLE-4-SULFONAMIDE, SULFATE ION, ... (6 entities in total)
• 機能のキーワード: receptor, agonist, antagonist
• 由来する生物種: HOMO SAPIENS (HUMAN)
• 細胞内の位置: Nucleus. Isoform A: Nucleus. Isoform 4: Mitochondrion outer membrane : P06401
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 61170.95

構造登録者

Lusher, S.J.,Raaijmakers, H.C.A.,Vu-Pham, D.,Dechering, K.,Wai Lam, T.,Brown, A.R.,Hamilton, N.M.,Nimz, O.,Azevedo, R.,Mcguire, R.,Oubrie, A.,de Vlieg, J. (登録日: 2011-06-15, 公開日: 2011-08-17, 最終更新日: 2024-05-08)

主引用文献

Lusher, S.J.,Raaijmakers, H.C.,Vu-Pham, D.,Dechering, K.,Lam, T.W.,Brown, A.R.,Hamilton, N.M.,Nimz, O.,Bosch, R.,McGuire, R.,Oubrie, A.,de Vlieg, J.
Structural basis for agonism and antagonism for a set of chemically related progesterone receptor modulators.
J. Biol. Chem., 286:35079-35086, 2011

PubMed Abstract: The progesterone receptor is able to bind to a large number and variety of ligands that elicit a broad range of transcriptional responses ranging from full agonism to full antagonism and numerous mixed profiles inbetween. We describe here two new progesterone receptor ligand binding domain x-ray structures bound to compounds from a structurally related but functionally divergent series, which show different binding modes corresponding to their agonistic or antagonistic nature. In addition, we present a third progesterone receptor ligand binding domain dimer bound to an agonist in monomer A and an antagonist in monomer B, which display binding modes in agreement with the earlier observation that agonists and antagonists from this series adopt different binding modes.

PubMed: 21849509
DOI: 10.1074/jbc.M111.273029

実験手法

X-RAY DIFFRACTION (1.8 Å)