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However, the applications of PROTACs as heterobifunctional molecules are largely limited by high molecular weight, low bioavailability, poor permeability, insufficient targeting, and low efficacy in vivo. Herein, self\u2010assembling micelles of FA\u2010PEG\u2010PROTAC are designed for cancer cell selective targeting and reductive\u2010response proteolysis in tumor\u2010bearing mice. FA\u2010PEG\u2010PROTAC is prepared by conjugating folic acid (FA)\u2010PEG with EGFR\u2010targeting PROTAC via a disulfide bond. The FA\u2010PEG\u2010PROTAC micelles, formed by self\u2010assembling, are demonstrated to significantly improve tumor targeting efficacy and exhibit excellent anti\u2010tumor efficacy in the mouse xenograft model compared to the traditional PROTACs. The strategy of applying self\u2010assembled FA\u2010PEG\u2010PROTAC micelles in tumor therapy can not only improve targeted proteolysis efficiency but also broaden applications in the development of PROTAC\u2010based drugs.<\/jats:p>","DOI":"10.1002\/adhm.202400109","type":"journal-article","created":{"date-parts":[[2024,4,27]],"date-time":"2024-04-27T05:38:45Z","timestamp":1714196325000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":42,"title":["Folate\u2010PEG\u2010PROTAC Micelles for Enhancing Tumor\u2010Specific Targeting Proteolysis In Vivo"],"prefix":"10.1002","volume":"13","author":[{"given":"Junhui","family":"Ma","sequence":"first","affiliation":[{"name":"Department of Pharmacy Tongji Medical College Huazhong University of Science and Technology  Wuhan 430030 China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lei","family":"Fang","sequence":"additional","affiliation":[{"name":"Department of 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