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Three Roundsnof Stability-Guided Optimization andnSystematical Evaluation of Oncolytic Peptide LTX-315 溶瘤肽LTX-315的三轮非稳定性优化及系统评价

Figshare Pub Date : 2024-01-26 DOI: 10.1021/acs.jmedchem.3c02232.s001

Xing-Yan Fu (17857861), Hao Yin (381910), Xi-Tong Chen (17857864), Jing-Fang Yao (17857867), Yan-Nan Ma (17857870), Min Song (57124), Huan Xu (38476), Qian-Yao Yu (17857873), Shan-Shan Du (795062), Yun-Kun Qi (1838839), Ke-Wei Wang (11371533)

{"title":"Three Roundsnof Stability-Guided Optimization andnSystematical Evaluation of Oncolytic Peptide LTX-315","authors":"Xing-Yan Fu (17857861), Hao Yin (381910), Xi-Tong Chen (17857864), Jing-Fang Yao (17857867), Yan-Nan Ma (17857870), Min Song (57124), Huan Xu (38476), Qian-Yao Yu (17857873), Shan-Shan Du (795062), Yun-Kun Qi (1838839), Ke-Wei Wang (11371533)","doi":"10.1021/acs.jmedchem.3c02232.s001","DOIUrl":"https://doi.org/10.1021/acs.jmedchem.3c02232.s001","url":null,"abstract":"Oncolytic peptides represent promisingnnovel candidatesnfor anticancerntreatments. In our efforts to develop oncolytic peptides possessingnboth high protease stability and durable anticancer efficiency, threenrounds of optimization were conducted on the first-in-class oncolyticnpeptide LTX-315. The robust synthetic method, in vitro and in vivonanticancer activity, and anticancer mechanism were investigated. ThenD-type peptides represented by FXY-12 possessed significantly improvednproteolytic stability and sustained anticancer efficiency. Strikingly,nthe novel hybrid peptide FXY-30, containing one FXY-12 and two camptothecinnmoieties, exhibited the most potent in vitro and in vivo anticancernactivities. The mechanism explorations indicated that FXY-30 exhibitednrapid membranolytic effects and induced severe DNA double-strand breaksnto trigger cell apoptosis. Collectively, this study not only establishednrobust strategies to improve the stability and anticancer potentialnof oncolytic peptides but also provided valuable references for thenfuture development of D-type peptides-based hybrid anticancer chemotherapeutics.","PeriodicalId":523777,"journal":{"name":"Figshare","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147921776","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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