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PDBsum entry 4uv9
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protein ligands Protein-protein interface(s) links
Transcription PDB id
4uv9

 

 

 

 

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JSmol PyMol  
Contents
Protein chains
666 a.a.
133 a.a.
Ligands
D70
PDB id:
4uv9
Name: Transcription
Title: Lsd1(kdm1a)-corest in complex with 1-ethyl-tranylcypromine
Structure: Lysine-specific histone demethylase 1a. Chain: a. Synonym: braf35-hdac complex protein bhc110, flavin-containing amine oxidase domain-containing protein 2. Engineered: yes. Rest corepressor 1. Chain: b. Synonym: protein corest. Engineered: yes
Source: Homo sapiens. Human. Organism_taxid: 9606. Expressed in: escherichia coli. Expression_system_taxid: 511693.
Resolution:
3.00Å     R-factor:   0.227     R-free:   0.246
Authors: P.Vianello,O.Botrugno,A.Cappa,G.Ciossani,P.Dessanti,A.Mai,A.Mattevi, G.Meroni,S.Minucci,F.Thaler,M.Tortorici,P.Trifiro,S.Valente,M.Villa, M.Varasi,C.Mercurio
Key ref: P.Vianello et al. (2014). 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, 86, 352-363. PubMed id: 25173853 DOI: 10.1016/j.ejmech.2014.08.068
Date:
05-Aug-14     Release date:   10-Sep-14    
PROCHECK
Go to PROCHECK summary
 Headers
 References

Protein chain
Pfam   ArchSchema ?
O60341  (KDM1A_HUMAN) -  Lysine-specific histone demethylase 1A from Homo sapiens
Seq:
Struc: 		 
Seq:
Struc: 		852 a.a.
666 a.a.
Protein chain
Pfam   ArchSchema ?
Q9UKL0  (RCOR1_HUMAN) -  REST corepressor 1 from Homo sapiens
Seq:
Struc: 		485 a.a.
133 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 Enzyme reactions 
   Enzyme class: Chain A: E.C.1.14.99.66  - [histone-H3]-N(6),N(6)-dimethyl-L-lysine(4) FAD-dependent demethylase.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction: N6,N6-dimethyl-L-lysyl4-[histone H3] + 2 A + 2 H2O = L-lysyl4- [histone H3] + 2 formaldehyde + 2 AH2
N(6),N(6)-dimethyl-L-lysyl(4)-[histone H3]
 + 2 × A
 + 2 × H2O
 = L-lysyl(4)- [histone H3]
 + 2 × formaldehyde
 + 2 × AH2
Molecule diagrams generated from .mol files obtained from the KEGG ftp site

 

 
    Key reference    
 
 
DOI no: 10.1016/j.ejmech.2014.08.068 Eur J Med Chem 86:352-363 (2014)
PubMed id: 25173853  
 
 
Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A.
P.Vianello, O.A.Botrugno, A.Cappa, G.Ciossani, P.Dessanti, A.Mai, A.Mattevi, G.Meroni, S.Minucci, F.Thaler, M.Tortorici, P.Trifiró, S.Valente, M.Villa, M.Varasi, C.Mercurio.
 
  ABSTRACT  
 
No abstract given.

 

 

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