7VNI

AHR-ARNT PAS-B heterodimer

7VNI の概要

• エントリーDOI: 10.2210/pdb7vni/pdb
• 分子名称: Ahr homolog spineless, Aryl hydrocarbon receptor nuclear translocator, SULFATE ION, ... (4 entities in total)
• 機能のキーワード: transcription factor, ligand binding domain, transcription
• 由来する生物種: Drosophila melanogaster (Fruit fly); 詳細
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 54107.26

構造登録者

Dai, S.Y. (登録日: 2021-10-11, 公開日: 2022-04-13, 最終更新日: 2023-11-29)

主引用文献

Dai, S.,Qu, L.,Li, J.,Zhang, Y.,Jiang, L.,Wei, H.,Guo, M.,Chen, X.,Chen, Y.
Structural insight into the ligand binding mechanism of aryl hydrocarbon receptor.
Nat Commun, 13:6234-6234, 2022

PubMed Abstract: The aryl hydrocarbon receptor (AHR), a member of the basic helix-loop-helix (bHLH) Per-Arnt-Sim (PAS) family of transcription factors, plays important roles in regulating xenobiotic metabolism, cellular differentiation, stem cell maintenance, as well as immunity. More recently, AHR has gained significant interest as a drug target for the development of novel cancer immunotherapy drugs. Detailed understanding of AHR-ligand binding has been hampered for decades by the lack of a three-dimensional structure of the AHR PAS-B domain. Here, we present multiple crystal structures of the Drosophila AHR PAS-B domain, including its apo, ligand-bound, and AHR nuclear translocator (ARNT) PAS-B-bound forms. Together with biochemical and cellular assays, our data reveal structural features of the AHR PAS-B domain, provide insights into the mechanism of AHR ligand binding, and provide the structural basis for the future development of AHR-targeted therapeutics.

PubMed: 36266304
DOI: 10.1038/s41467-022-33858-w

実験手法

X-RAY DIFFRACTION (1.997 Å)