4UVA

LSD1(KDM1A)-CoREST in complex with 1-Methyl-Tranylcypromine (1R,2S)

Summary for 4UVA

• Entry DOI: 10.2210/pdb4uva/pdb
• Related: 4UV8 4UV9 4UVB 4UVC
• Descriptor: LYSINE-SPECIFIC HISTONE DEMETHYLASE 1A, REST COREPRESSOR 1, [(2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl]methyl (2R,3S,4S)-2,3,4-trihydroxy-5-[(4aS)-4a-[(1S,3E)-3-imino-1-phenylbutyl]-7,8-dimethyl-2,4-dioxo-3,4,4a,5-tetrahydrobenzo[g]pteridin-10(2H)-yl]pentyl dihydrogen diphosphate, ... (4 entities in total)
• Functional Keywords: transcription, covalent inhibitor
• Biological source: HOMO SAPIENS (HUMAN); More
• Cellular location: Nucleus: O60341 Q9UKL0
• Total number of polymer chains: 2
• Total formula weight: 148880.96

Authors

Vianello, P.,Botrugno, O.,Cappa, A.,Ciossani, G.,Dessanti, P.,Mai, A.,Mattevi, A.,Meroni, G.,Minucci, S.,Thaler, F.,Tortorici, M.,Trifiro, P.,Valente, S.,Villa, M.,Varasi, M.,Mercurio, C. (deposition date: 2014-08-05, release date: 2014-09-10, Last modification date: 2024-01-10)

• Primary citation: Vianello, P.,Botrugno, O.A.,Cappa, A.,Ciossani, G.,Dessanti, P.,Mai, A.,Mattevi, A.,Meroni, G.,Minucci, S.,Thaler, F.,Tortorici, M.,Trifiro, P.,Valente, S.,Villa, M.,Varasi, M.,Mercurio, C.; Synthesis, Biological Activity and Mechanistic Insights of 1-Substituted Cyclopropylamine Derivatives: A Novel Class of Irreversible Inhibitors of Histone Demethylase Kdm1A.; Eur.J.Med.Chem., 86C:352-, 2014; PubMed: 25173853; DOI: 10.1016/J.EJMECH.2014.08.068

Experimental method

X-RAY DIFFRACTION (2.9 Å)