Advances in the design, discovery, and optimization of aurora kinase inhibitors as anticancer agents.

IF 6 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Expert Opinion on Drug Discovery Pub Date : 2025-04-01 Epub Date: 2025-03-31 DOI:10.1080/17460441.2025.2481272
Anubhav Verma, Pradhuman Bharatiya, Aashish Jaitak, Vaibhav Nigam, Vikramdeep Monga
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引用次数: 0

Abstract

Introduction: Aurora kinases (AKs) play key roles during carcinogenesis and show a close relationship with many cellular effects including mitotic entry, spindle assembly and chromosomal alignment biorientation. Indeed, elevated levels of AKs have been reported in several different tumor types, leading research scientists to investigate ways that we can target AKs for the purpose of developing new anticancer therapeutics.

Area covered: This review examines the design, discovery, and development of Aurora kinase inhibitors (AKIs) as anticancer agents and delineates their roles in cancer progression or development. Various databases like PubMed, Scopus, Google scholar, SciFinder were used to search the relevant information. This article provides a comprehensive overview of recent advances in the medicinal chemistry of AKIs including the candidates under clinical development and list of patents filed. In addition, their mechanistic findings, SARs, and in silico studies have also been discussed to offer prospects in this field.

Expert opinion: The integration of artificial intelligence and computational approaches is poised to accelerate the development of AKIs as anticancer agents. However, the associated challenges currently hindering its impact in drug development must be overcome before drugs can successfully translate from early drug development into clinical practice.

极光激酶抑制剂抗癌药物的设计、发现和优化进展。
奥罗拉激酶(Aurora激酶,AKs)在癌变过程中起着关键作用,并与许多细胞效应密切相关,包括有丝分裂进入、纺锤体组装和染色体双取向排列。事实上,在几种不同的肿瘤类型中都有AKs水平升高的报道,这使得研究科学家们开始研究我们可以针对AKs开发新的抗癌疗法的方法。涵盖领域:本文综述了极光激酶抑制剂(AKIs)作为抗癌药物的设计、发现和发展,并描述了它们在癌症进展或发展中的作用。使用PubMed、Scopus、b谷歌scholar、SciFinder等数据库检索相关信息。本文全面概述了AKIs药物化学的最新进展,包括临床开发中的候选药物和已提交的专利清单。此外,还讨论了他们的机制发现,sar和硅片研究,为该领域的发展提供了前景。专家意见:人工智能和计算方法的结合将加速AKIs作为抗癌药物的发展。然而,在药物成功地从早期药物开发转化为临床实践之前,必须克服目前阻碍其在药物开发中的影响的相关挑战。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
10.20
自引率
1.60%
发文量
78
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Drug Discovery (ISSN 1746-0441 [print], 1746-045X [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on novel technologies involved in the drug discovery process, leading to new leads and reduced attrition rates. Each article is structured to incorporate the author’s own expert opinion on the scope for future development. The Editors welcome: Reviews covering chemoinformatics; bioinformatics; assay development; novel screening technologies; in vitro/in vivo models; structure-based drug design; systems biology Drug Case Histories examining the steps involved in the preclinical and clinical development of a particular drug The audience consists of scientists and managers in the healthcare and pharmaceutical industry, academic pharmaceutical scientists and other closely related professionals looking to enhance the success of their drug candidates through optimisation at the preclinical level.
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