Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections

BRDT, BRD2, BRD3, and BRD4 comprise the bromodomain and extraterminal (BET) subfamily which contain two similar tandem bromodomains (BD1 and BD2). Selective BD1 inhibition phenocopies effects of tandem BET BD inhibition both in cancer models and, as we and others have reported of BRDT, in the testes...

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Detalles Bibliográficos
Autores principales: Modukuri, Ram K., Yu, Zhifeng, Tan, Zhi, Ta, Hai Minh, Ucisik, Melek Nihan, Jin, Zhuang, Anglin, Justin L., Sharma, Kiran L., Nyshadham, Pranavanand, Li, Feng, Riehle, Kevin, Faver, John C., Duong, Kevin, Nagarajan, Sureshbabu, Simmons, Nicholas, Palmer, Stephen S., Teng, Mingxing, Young, Damian W., Yi, Joanna S., Kim, Choel, Matzuk, Martin M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: National Academy of Sciences 2022
Materias:
Physical Sciences
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9295786/
https://www.ncbi.nlm.nih.gov/pubmed/35622893
http://dx.doi.org/10.1073/pnas.2122506119

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