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Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression
Proteins of the bromodomain and extra-terminal (BET) family are epigenetics “readers” and promising therapeutic targets for cancer and other human diseases. We describe herein a structure-guided design of 1,4-oxazepines as a new class of BET inhibitors and our subsequent design, synthesis and evalua...
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| 出版年: | J Med Chem |
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| 主要な著者: | , , , , , , , , , , , , , , , , , , , , , , |
| フォーマット: | Artigo |
| 言語: | Inglês |
| 出版事項: |
2018
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| 主題: | |
| オンライン・アクセス: | https://ncbi.nlm.nih.gov/pmc/articles/PMC6545111/ https://ncbi.nlm.nih.gov/pubmed/30019901 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b00506 |
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