9FWG

LSD1/CoREST bound to bomedemstat

This is a non-PDB format compatible entry.

Summary for 9FWG

• Entry DOI: 10.2210/pdb9fwg/pdb
• Descriptor: Lysine-specific histone demethylase 1A, REST corepressor 1, Bomedemstat FAD adduct (3 entities in total)
• Functional Keywords: bomedemstat, epigenetics, histone demethylase, oxidoreductase
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 2
• Total formula weight: 147350.52

Authors

Speranzini, V.,Mattevi, A. (deposition date: 2024-06-30, release date: 2024-07-10)

Primary citation

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

Experimental method

X-RAY DIFFRACTION (3.2 Å)