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Redefining Cancer Therapy: Toward BCL-XL/BCL-2 Dual Inhibitors with Diminished Platelet Toxicity.

Robert B Kargbo
Published in: ACS medicinal chemistry letters (2023)
This Patent Highlight focuses on the development of Bcl-xL/Bcl-2 dual inhibitors with minimized platelet toxicity to improve cancer treatment strategies. Acknowledging the critical role of antiapoptotic Bcl-2 family proteins in cancer pathogenesis, the paper reviews various inhibitors, notably venetoclax. Despite its success, resistance due to Bcl-xL upregulation prompted interest in dual inhibitors like ABT-263. However, their use often incurs platelet toxicity. Hence, this Patent Highlight showcases the synthesis of new compounds that could maintain potent antitumor effects while preserving platelet viability. This novel approach could redefine cancer therapy, offering more effective treatment for Bcl-2-driven cancers.
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