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Structure paper

TitleBiochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases Lsd1 and Lsd2.
Journal, issue, pagesJ. Am. Chem. Soc., Vol. 132, Page 6827-, Year 2010
Publish dateMar 31, 2010 (structure data deposition date)
AuthorsBinda, C. / Valente, S. / Romanenghi, M. / Pilotto, S. / Cirilli, R. / Karytinos, A. / Ciossani, G. / Botrugno, O.A. / Forneris, F. / Tardugno, M. ...Binda, C. / Valente, S. / Romanenghi, M. / Pilotto, S. / Cirilli, R. / Karytinos, A. / Ciossani, G. / Botrugno, O.A. / Forneris, F. / Tardugno, M. / Edmondson, D.E. / Minucci, S. / Mattevi, A. / Mai, A.
External linksJ. Am. Chem. Soc. / PubMed:20415477
MethodsX-ray diffraction
Resolution3.1 - 3.3 Å
Structure data

PDB-2xaf:
Crystal structure of LSD1-CoREST in complex with para-bromo-(+)-cis-2- phenylcyclopropyl-1-amine
Method: X-RAY DIFFRACTION / Resolution: 3.25 Å

PDB-2xag:
Crystal structure of LSD1-CoREST in complex with para-bromo-(-)-trans- 2-phenylcyclopropyl-1-amine
Method: X-RAY DIFFRACTION / Resolution: 3.1 Å

PDB-2xah:
Crystal structure of LSD1-CoREST in complex with (+)-trans-2- phenylcyclopropyl-1-amine
Method: X-RAY DIFFRACTION / Resolution: 3.1 Å

PDB-2xaj:
Crystal structure of LSD1-CoREST in complex with (-)-trans-2- phenylcyclopropyl-1-amine
Method: X-RAY DIFFRACTION / Resolution: 3.3 Å

PDB-2xaq:
Crystal structure of LSD1-CoREST in complex with a tranylcypromine derivative (MC2584, 13b)
Method: X-RAY DIFFRACTION / Resolution: 3.2 Å

PDB-2xas:
Crystal structure of LSD1-CoREST in complex with a tranylcypromine derivative (MC2580, 14e)
Method: X-RAY DIFFRACTION / Resolution: 3.2 Å

Chemicals

ChemComp-FAD:
FLAVIN-ADENINE DINUCLEOTIDE / FAD*YM

ChemComp-TCF:
3-(4-BROMOPHENYL)PROPANAMIDE

ChemComp-3PL:
3-PHENYLPROPANAL

ChemComp-TCA:
PHENYLETHYLENECARBOXYLIC ACID

ChemComp-M84:
3-{4-[(PHENYLCARBONYL)AMINO]PHENYL}PROPANOIC ACID

ChemComp-M80:
3-[4-({N-[(BENZYLOXY)CARBONYL]-L-PHENYLALANYL}AMINO)PHENYL]PROPANOIC ACID

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / AMINE OXIDASE / CHROMATIN REGULATOR / HISTONE INHIBITOR BINDING / METHYLATION / NUCLEOSOME CORE / OXIDOREDUCTASE / OXIDOREDUCTASE-REPRESSOR COMPLEX / CHROMATIN REMODELLING

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