spacer
spacer

PDBsum entry 4uvc
Go to PDB code: 
protein ligands Protein-protein interface(s) links
Transcription PDB id
4uvc

 

 

 

 

Loading ...

 
JSmol PyMol  
Contents
Protein chains
666 a.a.
133 a.a.
Ligands
D52
PDB id:
4uvc
Name: Transcription
Title: Lsd1(kdm1a)-corest in complex with 1-phenyl-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 bl21. Expression_system_taxid: 511693. Expression_system_taxid: 511693
Resolution:
3.10Å     R-factor:   0.211     R-free:   0.241
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.

 

 

spacer
spacer