M Amin Mir, Devalina Ray, Suman Mazumdar, Bimal Krishna Banik
{"title":"靶向癌症治疗的激酶抑制剂。","authors":"M Amin Mir, Devalina Ray, Suman Mazumdar, Bimal Krishna Banik","doi":"10.2174/0115680266382257250721051440","DOIUrl":null,"url":null,"abstract":"<p><p>Precision medicine's quick development has transformed the way cancer is treated, and because small-molecule kinase inhibitors can specifically block the abnormal signaling pathways that cause tumor growth and progression, they are now a key component of targeted therapy. This review explores the most recent advancements in kinase inhibitor design and optimization, with a focus on novel drug scaffolds, improved structure-activity relationships (SARs), and molecular modification techniques meant to improve target selectivity, potency, and pharmacokinetic profiles. Emerging strategies to combat resistance mechanisms are heavily emphasized, such as the use of dual-target inhibitors that block parallel signaling cascades, allosteric modulators that bind to non-ATP sites, and combination therapies that work in concert to increase efficacy while reducing resistance. A thorough summary of the kinase inhibitors that are now FDA-approved for use in treating different forms of cancer is also included in the review, along with information on their safety profiles, clinical effectiveness, and changing indications of usage. Additionally, it examines encouraging results from preclinical research and ongoing clinical studies assessing nextgeneration kinase inhibitors, which have the potential to further customize cancer treatment. In order to improve patient outcomes, address therapeutic resistance, and broaden the therapeutic scope of kinase-targeted interventions in oncology, the review concludes by highlighting future research directions, such as drug repurposing, computational drug discovery, and advanced precision oncology approaches.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3000,"publicationDate":"2025-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Kinase Inhibitors for Targeted Cancer Therapy.\",\"authors\":\"M Amin Mir, Devalina Ray, Suman Mazumdar, Bimal Krishna Banik\",\"doi\":\"10.2174/0115680266382257250721051440\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Precision medicine's quick development has transformed the way cancer is treated, and because small-molecule kinase inhibitors can specifically block the abnormal signaling pathways that cause tumor growth and progression, they are now a key component of targeted therapy. This review explores the most recent advancements in kinase inhibitor design and optimization, with a focus on novel drug scaffolds, improved structure-activity relationships (SARs), and molecular modification techniques meant to improve target selectivity, potency, and pharmacokinetic profiles. Emerging strategies to combat resistance mechanisms are heavily emphasized, such as the use of dual-target inhibitors that block parallel signaling cascades, allosteric modulators that bind to non-ATP sites, and combination therapies that work in concert to increase efficacy while reducing resistance. A thorough summary of the kinase inhibitors that are now FDA-approved for use in treating different forms of cancer is also included in the review, along with information on their safety profiles, clinical effectiveness, and changing indications of usage. Additionally, it examines encouraging results from preclinical research and ongoing clinical studies assessing nextgeneration kinase inhibitors, which have the potential to further customize cancer treatment. In order to improve patient outcomes, address therapeutic resistance, and broaden the therapeutic scope of kinase-targeted interventions in oncology, the review concludes by highlighting future research directions, such as drug repurposing, computational drug discovery, and advanced precision oncology approaches.</p>\",\"PeriodicalId\":11076,\"journal\":{\"name\":\"Current topics in medicinal chemistry\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":3.3000,\"publicationDate\":\"2025-07-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current topics in medicinal chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.2174/0115680266382257250721051440\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current topics in medicinal chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/0115680266382257250721051440","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Precision medicine's quick development has transformed the way cancer is treated, and because small-molecule kinase inhibitors can specifically block the abnormal signaling pathways that cause tumor growth and progression, they are now a key component of targeted therapy. This review explores the most recent advancements in kinase inhibitor design and optimization, with a focus on novel drug scaffolds, improved structure-activity relationships (SARs), and molecular modification techniques meant to improve target selectivity, potency, and pharmacokinetic profiles. Emerging strategies to combat resistance mechanisms are heavily emphasized, such as the use of dual-target inhibitors that block parallel signaling cascades, allosteric modulators that bind to non-ATP sites, and combination therapies that work in concert to increase efficacy while reducing resistance. A thorough summary of the kinase inhibitors that are now FDA-approved for use in treating different forms of cancer is also included in the review, along with information on their safety profiles, clinical effectiveness, and changing indications of usage. Additionally, it examines encouraging results from preclinical research and ongoing clinical studies assessing nextgeneration kinase inhibitors, which have the potential to further customize cancer treatment. In order to improve patient outcomes, address therapeutic resistance, and broaden the therapeutic scope of kinase-targeted interventions in oncology, the review concludes by highlighting future research directions, such as drug repurposing, computational drug discovery, and advanced precision oncology approaches.
期刊介绍:
Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.