靶向癌症治疗的激酶抑制剂。

IF 3.3 4区 医学 Q3 CHEMISTRY, MEDICINAL
M Amin Mir, Devalina Ray, Suman Mazumdar, Bimal Krishna Banik
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引用次数: 0

摘要

精准医学的快速发展已经改变了癌症的治疗方式,因为小分子激酶抑制剂可以特异性地阻断导致肿瘤生长和进展的异常信号通路,它们现在是靶向治疗的关键组成部分。这篇综述探讨了激酶抑制剂设计和优化的最新进展,重点是新的药物支架,改进的结构-活性关系(SARs),以及旨在提高靶标选择性,效价和药代动力学谱的分子修饰技术。本文着重强调了对抗耐药机制的新策略,如使用阻断平行信号级联的双靶点抑制剂,结合非atp位点的变构调节剂,以及协同作用以提高疗效同时降低耐药的联合治疗。对目前fda批准用于治疗不同类型癌症的激酶抑制剂的全面总结也包括在审查中,以及它们的安全性,临床有效性和使用适应症的变化信息。此外,它还检查了临床前研究和正在进行的评估下一代激酶抑制剂的临床研究的令人鼓舞的结果,这些研究有可能进一步定制癌症治疗。为了改善患者的治疗效果,解决治疗耐药问题,拓宽肿瘤中激酶靶向干预的治疗范围,本文总结了未来的研究方向,如药物再利用、计算药物发现和先进的精确肿瘤方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Kinase Inhibitors for Targeted Cancer Therapy.

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.

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来源期刊
CiteScore
6.40
自引率
2.90%
发文量
186
审稿时长
3-8 weeks
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.
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