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首页> 外文期刊>Breast Cancer: Targets and Therapy >Targeting γ-secretase in breast cancer
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Targeting γ-secretase in breast cancer

机译：靶向乳腺癌中的γ-分泌酶

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Abstract: γ-secretase complexes are multisubunit protease complexes that perform the intramembrane cleavage of more than 60 type-I transmembrane proteins, including Notch receptors. Since dysregulated Notch signaling has been implicated in the tumorigenesis and progression of breast cancer, small molecule γ-secretase inhibitors (GSIs) are being tested for their therapeutic potential in breast cancer treatment in several clinical trials. Here, the structure of γ-secretase complex and the development of GSIs are briefly reviewed, the roles of Notch and several other γ-secretase substrates in breast cancer are discussed, and the difference between γ-secretase inhibition and Notch inhibition, as well as the side effects associated with GSIs, are described. A better understanding of molecular mechanisms that affect the responsiveness of breast cancer to GSI might help to develop strategies to enhance the antitumor activity and, at the same time, alleviate the side effects of GSI.
机译：摘要：γ-分泌酶复合物是多亚基蛋白酶复合物，可对包括Notch受体在内的60多种I型跨膜蛋白进行膜内切割。由于Notch信号传导异常与乳腺癌的发生和发展有关，因此在一些临床试验中，正在测试小分子γ-分泌酶抑制剂（GSI）在乳腺癌治疗中的治疗潜力。在此，简要回顾了γ-分泌酶复合物的结构和GSI的发展，探讨了Notch和其他几种γ-分泌酶底物在乳腺癌中的作用，以及γ-分泌酶抑制和Notch抑制之间的区别，以及描述了与GSI相关的副作用。更好地了解影响乳腺癌对GSI响应的分子机制可能有助于制定增强抗肿瘤活性的策略，同时减轻GSI的副作用。

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