Advances in targeted delivery of proteolysis targeting chimeras in cancer therapy].

Xiaobo Wu, Jie Zhao, Yuan Gao, Qingxin Yao, Jianjun Xie

Sheng wu gong cheng xue bao = Chinese journal of biotechnology 2023 Sep 25

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Small-molecule anticancer drugs inhibited tumor growth based on targeted inhibition of specific proteins, while most of oncogenic proteins are "undruggable". Proteolysis targeting chimeras (PROTAC) is an attractive and general strategy for treating cancer based on targeted degradation of oncogenic proteins. This review briefly describes the peptide-based PTOTAC and small molecule-based PROTAC. Subsequently, we summarize the development of targeted delivery of PROTAC, such as targeting molecule-mediated targeted delivery of PROTAC, nanomaterial-mediated targeted delivery of PROTAC and controllable activation of small-molecular PROTAC prodrug. Such strategies show potential application in improving tumor selectivity, overcoming off-target effect and reducing biotoxicity. At the end, the druggability of PROTAC is prospected.

Citation

Xiaobo Wu, Jie Zhao, Yuan Gao, Qingxin Yao, Jianjun Xie. Advances in targeted delivery of proteolysis targeting chimeras in cancer therapy]. Sheng wu gong cheng xue bao = Chinese journal of biotechnology. 2023 Sep 25;39(9):3628-3643