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Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies

[Image: see text] SET domain-containing protein 2 (SETD2), a histone methyltransferase, has been identified as a target of interest in certain hematological malignancies, including multiple myeloma. This account details the discovery of EPZ-719, a novel and potent SETD2 inhibitor with a high selecti...

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Detalles Bibliográficos
Autores principales: Lampe, John W., Alford, Joshua S., Boriak-Sjodin, P. Ann, Brach, Dorothy, Cosmopoulos, Kat, Duncan, Kenneth W., Eckley, Sean T., Foley, Megan A., Harvey, Darren M., Motwani, Vinny, Munchhof, Michael J., Raimondi, Alejandra, Riera, Thomas V., Tang, Cuyue, Thomenius, Michael J., Totman, Jennifer, Farrow, Neil A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8521618/
https://www.ncbi.nlm.nih.gov/pubmed/34671445
http://dx.doi.org/10.1021/acsmedchemlett.1c00272