9FWG

LSD1/CoREST bound to bomedemstat

これはPDB形式変換不可エントリーです。

9FWG の概要

• エントリーDOI: 10.2210/pdb9fwg/pdb
• 分子名称: Lysine-specific histone demethylase 1A, REST corepressor 1, Bomedemstat FAD adduct (3 entities in total)
• 機能のキーワード: bomedemstat, epigenetics, histone demethylase, oxidoreductase
• 由来する生物種: Homo sapiens (human); 詳細
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 147350.52

構造登録者

Speranzini, V.,Mattevi, A. (登録日: 2024-06-30, 公開日: 2024-07-10)

主引用文献

Jasmine, S.,Mandl, A.,Krueger, T.E.G.,Dalrymple, S.L.,Antony, L.,Dias, J.,Celatka, C.A.,Tapper, A.E.,Kleppe, M.,Kanayama, M.,Jing, Y.,Speranzini, V.,Wang, Y.Z.,Luo, J.,Trock, B.J.,Denmeade, S.R.,Carducci, M.A.,Mattevi, A.,Rienhoff, H.Y.,Isaacs, J.T.,Brennen, W.N.
Characterization of structural, biochemical, pharmacokinetic, and pharmacodynamic properties of the LSD1 inhibitor bomedemstat in preclinical models.
Prostate, 84:909-921, 2024

PubMed Abstract: Lysine-specific demethylase 1 (LSD1) is emerging as a critical mediator of tumor progression in metastatic castration-resistant prostate cancer (mCRPC). Neuroendocrine prostate cancer (NEPC) is increasingly recognized as an adaptive mechanism of resistance in mCRPC patients failing androgen receptor axis-targeted therapies. Safe and effective LSD1 inhibitors are necessary to determine antitumor response in prostate cancer models. For this reason, we characterize the LSD1 inhibitor bomedemstat to assess its clinical potential in NEPC as well as other mCRPC pathological subtypes.

PubMed: 38619005
DOI: 10.1158/1078-0432.CCR-20-2380

実験手法

X-RAY DIFFRACTION (3.2 Å)