Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity

The histone methyltransferase EZH2 has been the target of numerous small-molecule inhibitor discovery efforts over the last 10+ years. Emerging clinical data have provided early evidence for single agent activity with acceptable safety profiles for first-generation inhibitors. We have developed kine...

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Detalles Bibliográficos
Autores principales: Stuckey, Jacob I., Cantone, Nico R., Côté, Alexandre, Arora, Shilpi, Vivat, Valerie, Ramakrishnan, Ashwin, Mertz, Jennifer A., Khanna, Avinash, Brenneman, Jehrod, Gehling, Victor S., Moine, Ludivine, Sims, Robert J., Audia, James E., Trojer, Patrick, Levell, Julian R., Cummings, Richard T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Society for Biochemistry and Molecular Biology 2021
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7949150/
https://www.ncbi.nlm.nih.gov/pubmed/33524394
http://dx.doi.org/10.1016/j.jbc.2021.100349

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7949150/
https://www.ncbi.nlm.nih.gov/pubmed/33524394
http://dx.doi.org/10.1016/j.jbc.2021.100349

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