{"title":"还原性活化的CPP-PROTAC纳米复合物通过有效的细胞摄取增强目标降解。","authors":"Maho Miyamoto, Kosuke Saito, Hidetomo Yokoo, Yosuke Demizu","doi":"10.1039/d5cb00196j","DOIUrl":null,"url":null,"abstract":"<p><p>We developed a nanoparticle based on a cell-penetrating peptide-PROTAC conjugate with a disulfide linker, <i>MZ1-R9</i>, and dextran sulfate, enhancing cellular uptake and BRD4 degradation. This delivery platform significantly improves PROTAC bioavailability and offers a promising strategy to overcome membrane permeability challenges for targeted protein degradation.</p>","PeriodicalId":40691,"journal":{"name":"RSC Chemical Biology","volume":" ","pages":""},"PeriodicalIF":3.1000,"publicationDate":"2025-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12394912/pdf/","citationCount":"0","resultStr":"{\"title\":\"Reductively activated CPP-PROTAC nanocomplexes enhance target degradation <i>via</i> efficient cellular uptake.\",\"authors\":\"Maho Miyamoto, Kosuke Saito, Hidetomo Yokoo, Yosuke Demizu\",\"doi\":\"10.1039/d5cb00196j\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>We developed a nanoparticle based on a cell-penetrating peptide-PROTAC conjugate with a disulfide linker, <i>MZ1-R9</i>, and dextran sulfate, enhancing cellular uptake and BRD4 degradation. This delivery platform significantly improves PROTAC bioavailability and offers a promising strategy to overcome membrane permeability challenges for targeted protein degradation.</p>\",\"PeriodicalId\":40691,\"journal\":{\"name\":\"RSC Chemical Biology\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":3.1000,\"publicationDate\":\"2025-08-25\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12394912/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"RSC Chemical Biology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1039/d5cb00196j\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"RSC Chemical Biology","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1039/d5cb00196j","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
We developed a nanoparticle based on a cell-penetrating peptide-PROTAC conjugate with a disulfide linker, MZ1-R9, and dextran sulfate, enhancing cellular uptake and BRD4 degradation. This delivery platform significantly improves PROTAC bioavailability and offers a promising strategy to overcome membrane permeability challenges for targeted protein degradation.
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