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PROTAC: Harnessing Targeted Chimeras for Selective BCL-2 Degradation in Cancer Treatment

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ACS MEDICINAL CHEMISTRY LETTERS
卷 14, 期 5, 页码 541-542

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AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.3c00113

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The BCL-2 protein family members, such as BCL-2, BCL-XL, and MCL-1, have shown promise as therapeutic targets for cancer treatment, exemplified by the FDA approval of venetoclax in 2016. Scientists are actively working on designing analogs with improved pharmacokinetics and pharmacodynamics. This Patent Highlight presents PROTAC compounds that effectively and selectively degrade BCL-2, offering potential applications in cancer treatment, autoimmune disorders, and immune system diseases.
The anti-apoptotic BCL-2 protein family members, including BCL-2, BCL-XL, and MCL-1, have been established as promising therapeutic targets for cancer treatment, as evidenced by the FDA approval of venetoclax in 2016. Researchers have redoubled their efforts to design analogs that exhibit enhanced pharmacokinetic and pharmacodynamic characteristics. This Patent Highlight features PROTAC compounds that demonstrate potent and selective BCL-2 degradation, with potential applications in the treatment of cancer, autoimmune disorders, and immune system diseases.

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