5D75

Crystal structure of Human FKBD25 in complex with FK506

5D75 の概要

• エントリーDOI: 10.2210/pdb5d75/pdb
• 分子名称: Peptidyl-prolyl cis-trans isomerase FKBP3, 8-DEETHYL-8-[BUT-3-ENYL]-ASCOMYCIN, O-(O-(2-AMINOPROPYL)-O'-(2-METHOXYETHYL)POLYPROPYLENE GLYCOL 500), ... (4 entities in total)
• 機能のキーワード: fk506, fkbp25, fkbp3, immunophilin, inhibitor, isomerase-inhibitor complex, isomerase/inhibitor
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 16030.78

構造登録者

Rajan, S.,Prakash, A.,Yoon, H.S. (登録日: 2015-08-13, 公開日: 2016-04-06, 最終更新日: 2023-11-08)

主引用文献

Prakash, A.,Rajan, S.,Yoon, H.S.
Crystal structure of the FK506 binding domain of human FKBP25 in complex with FK506.
Protein Sci., 25:905-910, 2016

PubMed Abstract: Human FKBP25 (hFKBP25) is a nuclear immunophilin and interacts with several nuclear proteins, hence involving in many nuclear events. Similar to other FKBPs, FK506 binding domain (FKBD) of hFKBP25 also binds to immunosuppressive drugs such as rapamycin and FK506, albeit with a lower affinity for the latter. The molecular basis underlying this difference in affinity could not be addressed due to the lack of the crystal structure of hFKBD25 in complex with FK506. Here, we report the crystal structure of hFKBD25 in complex with FK506 determined at 1.8 Å resolution and its comparison with the hFKBD25-rapamycin complex, bringing out the microheterogeneity in the mode of interaction of these drugs, which could possibly explain the lower affinity for FK506.

PubMed: 26749369
DOI: 10.1002/pro.2875

実験手法

X-RAY DIFFRACTION (1.83 Å)