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Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.
England, Katherine S; Tumber, Anthony; Krojer, Tobias; Scozzafava, Giuseppe; Ng, Stanley S; Daniel, Michelle; Szykowska, Aleksandra; Che, KaHing; von Delft, Frank; Burgess-Brown, Nicola A; Kawamura, Akane; Schofield, Christopher J; Brennan, Paul E.
Afiliación
  • England KS; Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK.
  • Tumber A; Chemistry Research Laboratory, University of Oxford, Mansfield Road, Oxford, OX1 3TA, UK.
  • Krojer T; Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK.
  • Scozzafava G; Target Discovery Institute, University of Oxford, NDM Research Building, Roosevelt Drive, Oxford, OX3 7FZ, UK.
  • Ng SS; Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK.
  • Daniel M; Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK.
  • Szykowska A; Target Discovery Institute, University of Oxford, NDM Research Building, Roosevelt Drive, Oxford, OX3 7FZ, UK.
  • Che K; Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK.
  • von Delft F; Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK.
  • Burgess-Brown NA; Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK.
  • Kawamura A; Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK.
  • Schofield CJ; Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK.
  • Brennan PE; Diamond Light Source Ltd, Harwell Science and Innovation Campus, Didcot, OX11 0QX, UK.
Medchemcomm ; 5(12): 1879-1886, 2014 Dec 01.
Article en En | MEDLINE | ID: mdl-26682034
ABSTRACT
A potent inhibitor of the JmjC histone lysine demethylase KDM2A (compound 35, pIC50 7.2) with excellent selectivity over representatives from other KDM subfamilies has been developed; the discovery that a triazolopyridine compound binds to the active site of JmjC KDMs was followed by optimisation of the triazole substituent for KDM2A inhibition and selectivity.
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Texto completo: 1 Base de datos: MEDLINE Idioma: En Revista: Medchemcomm Año: 2014 Tipo del documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Base de datos: MEDLINE Idioma: En Revista: Medchemcomm Año: 2014 Tipo del documento: Article