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Novel BET protein Proteolysis Targeting Chimera (BET-PROTAC) exerts superior lethal activity than Bromodomain Inhibitor (BETi) against post-myeloproliferative Neoplasm (MPN) Secondary (s) AML Cells
The PROTAC (proteolysis-targeting chimera) ARV-825 recruits bromodomain and extraterminal (BET) proteins to the E3 ubiquitin ligase cereblon, leading to degradation of BET proteins, including BRD4. Whereas the BET-protein inhibitor (BETi) OTX015 caused accumulation of BRD4, treatment with equimolar...
Autores principales: | Saenz, Dyana T., Fiskus, Warren, Qian, Yimin, Manshouri, Taghi, Rajapakshe, Kimal, Raina, Kanak, Coleman, Kevin G., Crew, Andrew P., Shen, Angela, Mill, Christopher P., Sun, Baohua, Qiu, Peng, Kadia, Tapan M., Pemmaraju, Naveen, DiNardo, Courtney, Kim, Mi-Sun, Nowak, Agnieszka J., Coarfa, Cristian, Crews, Craig M., Verstovsek, Srdan, Bhalla, Kapil N. |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5537055/ https://www.ncbi.nlm.nih.gov/pubmed/28042144 http://dx.doi.org/10.1038/leu.2016.393 |
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