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首页> 外文期刊>Journal of Medicinal Chemistry >Pharmacological Targeting of Executioner Proteins: Controlling Life and Death
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Pharmacological Targeting of Executioner Proteins: Controlling Life and Death

机译：刽子手蛋白的药理靶向：控制生死

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Small-molecule mediated modulation of protein interactions of Bcl-2 (B-cell lymphoma-2) family proteins was clinically validated in 2015 when Venetoclax, a selective inhibitor of the antiapoptotic protein BCL-2, achieved breakthrough status designation by the FDA for treatment of lymphoid malignancies. Since then, substantial progress has been made in identifying inhibitors of other interactions of antiapoptosis proteins. However, targeting their pro-apoptotic counterparts, the "executioners" BAX, BAK, and BOK that both initiate and commit the cell to dying, has lagged behind. However, recent publications demonstrate that these proteins can be positively or negatively regulated using small molecule tool compounds. The results obtained with these molecules suggest that pharmaceutical regulation of apoptosis will have broad implications that extend beyond activating cell death in cancer. We review recent advances in identifying compounds and their utility in the exogenous control of life and death by regulating executioner proteins, with emphasis on the prototype BAX.
机译：2015年，当抗凋亡蛋白Bcl-2的选择性抑制剂Venetoclax获得FDA针对淋巴恶性肿瘤治疗的突破性地位时，Bcl-2（B细胞淋巴瘤-2）家族蛋白质相互作用的小分子介导调节在临床上得到验证。自那时以来，在识别抗凋亡蛋白的其他相互作用的抑制剂方面取得了实质性进展。然而，以促凋亡的对应物为目标的“刽子手”BAX、BAK和BOK启动并使细胞死亡，却落在了后面。然而，最近的出版物表明，这些蛋白质可以使用小分子工具化合物进行正调控或负调控。从这些分子中获得的结果表明，药物对细胞凋亡的调节将具有广泛的意义，其范围不仅限于激活癌症中的细胞死亡。我们回顾了近年来在鉴定化合物方面的进展，以及它们在通过调节刽子手蛋白质外源性控制生命和死亡方面的应用，重点介绍了原型BAX。

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