7F2J

Crystal structure of AtFKBP53 FKBD in complex with rapamycin

7F2J の概要

• エントリーDOI: 10.2210/pdb7f2j/pdb
• 関連するPDBエントリー: 6J2M
• 分子名称: Peptidyl-prolyl cis-trans isomerase FKBP53, RAPAMYCIN IMMUNOSUPPRESSANT DRUG, SULFATE ION, ... (5 entities in total)
• 機能のキーワード: fkbp, rapamycin, dimerization, isomerase
• 由来する生物種: Arabidopsis thaliana (Mouse-ear cress)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 29712.25

構造登録者

Singh, A.K.,Saharan, K.,Vasudevan, D. (登録日: 2021-06-11, 公開日: 2022-03-09, 最終更新日: 2023-11-29)

主引用文献

Singh, A.K.,Saharan, K.,Baral, S.,Luan, S.,Vasudevan, D.
Crystal packing reveals rapamycin-mediated homodimerization of an FK506-binding domain.
Int.J.Biol.Macromol., 206:670-680, 2022

PubMed Abstract: Chemically induced dimerization (CID) is used to induce proximity and result in artificial complex formation between a pair of proteins involved in biological processes in cells to investigate and regulate these processes. The induced heterodimerization of FKBP fusion proteins by rapamycin and FK506 has been extensively exploited as a chemically induced dimerization system to regulate and understand highly dynamic cellular processes. Here, we report the crystal structure of the AtFKBP53 FKBD in complex with rapamycin. The crystal packing reveals an unusual feature whereby two rapamycin molecules appear to mediate homodimerization of the FKBD. The triene arm of rapamycin appears to play a significant role in forming this dimer. This forms the first structural report of rapamycin-mediated homodimerization of an FKBP. The structural information on the rapamycin-mediated FKBD dimerization may be employed to design and synthesize covalently linked dimeric rapamycin, which may subsequently serve as a chemically induced dimerization system for the regulation and characterization of cellular processes.

PubMed: 35218805
DOI: 10.1016/j.ijbiomac.2022.02.107

実験手法

X-RAY DIFFRACTION (1.6 Å)