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...

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Publicado no:Leukemia
Main Authors: 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.
Formato: Artigo
Idioma:Inglês
Publicado em: 2017
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5537055/
https://ncbi.nlm.nih.gov/pubmed/28042144
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/leu.2016.393
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