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Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294

We present the crystal structure of the catalytic SET domain of G9a-like protein (GLP) in complex with BIX-01294. The inhibitor is bound in the substrate peptide groove at the location where the histone H3 residues (Lys4 to Arg8) N-terminal to the target lysine would occupy. The inhibitor is positio...

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Detalles Bibliográficos
Autores principales: Chang, Yanqi, Zhang, Xing, Horton, John R., Upadhyay, Anup K., Spannhoff, Astrid, Liu, Jin, Snyder, James P., Bedford, Mark T., Cheng, Xiaodong
Formato: Texto
Lenguaje:English
Publicado: 2009
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2676930/
https://www.ncbi.nlm.nih.gov/pubmed/19219047
http://dx.doi.org/10.1038/nsmb.1560