C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one series was designed to rationally exploit these residue differences between the histone substrate binding sites in order...

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Detalles Bibliográficos
Autores principales: Le Bihan, Yann-Vaï, Lanigan, Rachel M., Atrash, Butrus, McLaughlin, Mark G., Velupillai, Srikannathasan, Malcolm, Andrew G., England, Katherine S., Ruda, Gian Filippo, Mok, N. Yi, Tumber, Anthony, Tomlin, Kathy, Saville, Harry, Shehu, Erald, McAndrew, Craig, Carmichael, LeAnne, Bennett, James M., Jeganathan, Fiona, Eve, Paul, Donovan, Adam, Hayes, Angela, Wood, Francesca, Raynaud, Florence I., Fedorov, Oleg, Brennan, Paul E., Burke, Rosemary, van Montfort, Rob L.M., Rossanese, Olivia W., Blagg, Julian, Bavetsias, Vassilios
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Editions Scientifiques Elsevier 2019
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6580095/
https://www.ncbi.nlm.nih.gov/pubmed/31158747
http://dx.doi.org/10.1016/j.ejmech.2019.05.041

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