{"title":"克服对FLT3-ITD疗法的耐药性","authors":"Campbell McInnes","doi":"10.1021/acs.jmedchem.4c02878","DOIUrl":null,"url":null,"abstract":"FLT3-ITD (internal tandem duplication) is a key driver of acute myeloid leukemia (AML), and several FDA-approved drugs target this mutant kinase. This Viewpoint describes the discovery of inhibitors targeting point mutants and the development of SILA123, a highly potent and selective type II FLT3 inhibitor. In <i>in vivo</i> studies, SILA-123 significantly suppressed tumor growth in allograft models, demonstrating its potential in treating resistant AML.","PeriodicalId":46,"journal":{"name":"Journal of Medicinal Chemistry","volume":"233 1","pages":""},"PeriodicalIF":6.8000,"publicationDate":"2024-12-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Overcoming Resistance to FLT3-ITD Therapeutics\",\"authors\":\"Campbell McInnes\",\"doi\":\"10.1021/acs.jmedchem.4c02878\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"FLT3-ITD (internal tandem duplication) is a key driver of acute myeloid leukemia (AML), and several FDA-approved drugs target this mutant kinase. This Viewpoint describes the discovery of inhibitors targeting point mutants and the development of SILA123, a highly potent and selective type II FLT3 inhibitor. In <i>in vivo</i> studies, SILA-123 significantly suppressed tumor growth in allograft models, demonstrating its potential in treating resistant AML.\",\"PeriodicalId\":46,\"journal\":{\"name\":\"Journal of Medicinal Chemistry\",\"volume\":\"233 1\",\"pages\":\"\"},\"PeriodicalIF\":6.8000,\"publicationDate\":\"2024-12-12\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Medicinal Chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1021/acs.jmedchem.4c02878\",\"RegionNum\":1,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1021/acs.jmedchem.4c02878","RegionNum":1,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
FLT3-ITD (internal tandem duplication) is a key driver of acute myeloid leukemia (AML), and several FDA-approved drugs target this mutant kinase. This Viewpoint describes the discovery of inhibitors targeting point mutants and the development of SILA123, a highly potent and selective type II FLT3 inhibitor. In in vivo studies, SILA-123 significantly suppressed tumor growth in allograft models, demonstrating its potential in treating resistant AML.
期刊介绍：
The Journal of Medicinal Chemistry is a prestigious biweekly peer-reviewed publication that focuses on the multifaceted field of medicinal chemistry. Since its inception in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry, it has evolved to become a cornerstone in the dissemination of research findings related to the design, synthesis, and development of therapeutic agents.
The Journal of Medicinal Chemistry is recognized for its significant impact in the scientific community, as evidenced by its 2022 impact factor of 7.3. This metric reflects the journal's influence and the importance of its content in shaping the future of drug discovery and development. The journal serves as a vital resource for chemists, pharmacologists, and other researchers interested in the molecular mechanisms of drug action and the optimization of therapeutic compounds.
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