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

Xiaobo WU; Jie Zhao; Yuan Gao; Qingxin Yao; Jianjun Xie

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

Author: Xiaobo WU ¹ ; Jie ZHAO ¹ ; Yuan GAO ² ; Qingxin YAO ² ; Jianjun XIE ¹
Author Information

1. School of Materials Science and Engineering, Central South University of Forestry and Technology, Changsha 410004, Hunan, China.
2. CAS Key Laboratory for Biomedical Effects of Nanomaterials & Nanosafety, National Center for Nanoscience and Technology, Beijing 100190, China.
Publication Type:Journal Article
Keywords: anticancer drugs; cancer; protein degrades; proteolysis targeting chimeras; targeted delivery
MeSH: Humans; Proteolysis Targeting Chimera; Nanostructures; Neoplasms/drug therapy*; Proteolysis
From: Chinese Journal of Biotechnology 2023;39(9):3628-3643
CountryChina
Language:Chinese
Abstract: 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.