8FQJ

LSD1-CoREST in complex with T14, short soaking

Summary for 8FQJ

• Entry DOI: 10.2210/pdb8fqj/pdb
• Descriptor: Lysine-specific histone demethylase 1A, REST corepressor 1, [(2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl (2S,3R,4R)-2,3,4-trihydroxy-5-[(1R,3S,3aS,13R)-1-hydroxy-10,11-dimethyl-3-{4-[(5-methyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl}-4,6-dioxo-2,3,5,6-tetrahydro-1H-benzo[g]pyrrolo[2,1-e]pteridin-8(4H)-yl]pentyl dihydrogen diphosphate (3 entities in total)
• Functional Keywords: epigenetics, histone demethylase, drug resistance, covalent inhibitor, oxidoreductase
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 2
• Total formula weight: 112572.25

Authors

Caroli, J.,Mattevi, A. (deposition date: 2023-01-06, release date: 2024-06-26)

• Primary citation: Caroli, J.,Mattevi, A.; Distal drug resistance mutations promote covalent inhibitor-adduct Grob fragmentation in LSD1; To be published,

Experimental method

X-RAY DIFFRACTION (2.9 Å)