7EQV

Crystal structure of JMJD2A complexed with 3,4-dihydroxybenzoic acid

7EQV の概要

• エントリーDOI: 10.2210/pdb7eqv/pdb
• 分子名称: Lysine-specific demethylase 4A, 3,4-DIHYDROXYBENZOIC ACID, NICKEL (II) ION, ... (6 entities in total)
• 機能のキーワード: human histone lysine demethylase 4a, lysine-specific demethylase 4a, kdm4a, jmjd2a, 3, 4-dihydroxybenzoic acid, inhibitor, oxidoreductase
• 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: 40887.01

構造登録者

Fang, W.-K.,Yang, S.-M.,Wang, W.-C. (登録日: 2021-05-04, 公開日: 2022-05-18, 最終更新日: 2023-11-29)

主引用文献

Liu, J.S.,Fang, W.K.,Yang, S.M.,Wu, M.C.,Chen, T.J.,Chen, C.M.,Lin, T.Y.,Liu, K.L.,Wu, C.M.,Chen, Y.C.,Chuu, C.P.,Wang, L.Y.,Hsieh, H.P.,Kung, H.J.,Wang, W.C.
Natural product myricetin is a pan-KDM4 inhibitor which with poly lactic-co-glycolic acid formulation effectively targets castration-resistant prostate cancer.
J.Biomed.Sci., 29:29-29, 2022

PubMed Abstract: Castration-resistant prostate cancer (CRPC) with sustained androgen receptor (AR) signaling remains a critical clinical challenge, despite androgen depletion therapy. The Jumonji C-containing histone lysine demethylase family 4 (KDM4) members, KDM4A‒KDM4C, serve as critical coactivators of AR to promote tumor growth in prostate cancer and are candidate therapeutic targets to overcome AR mutations/alterations-mediated resistance in CRPC.

PubMed: 35534851
DOI: 10.1186/s12929-022-00812-3

実験手法

X-RAY DIFFRACTION (2.6 Å)