治疗癌症的小分子 CDK4/6 抑制剂专利回顾:2020 年至今。

IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Expert Opinion on Therapeutic Patents Pub Date : 2024-09-01 Epub Date: 2024-07-17 DOI:10.1080/13543776.2024.2379926
Xiaoling Huang, Shidi Xu, Lei Duan, Shan Xu, Wufu Zhu
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引用次数: 0

摘要

简介细胞周期蛋白依赖性蛋白激酶4/6(CDK4/6)是一类丝氨酸/苏氨酸蛋白激酶,在细胞周期调控中发挥着关键作用。CDK4/6在乳腺癌、黑色素瘤和非小细胞肺癌(NSCLC)等癌症中高度表达。目前,已开发出多种 CDK4/6 抑制剂,旨在开发有效的抑制剂来解决 CDK4/6 的耐药性和毒性问题:本文通过Espacenet检索专利,回顾了被广泛研究的CDK抑制剂和FDA批准的CDK4/6抑制剂的发展情况,以及2020年至今对CDK4/6具有良好抑制活性的专利抑制剂的最新进展:CDK4/6在许多肿瘤中高表达,已成为重要的抗肿瘤靶点。在2020年至今的专利中,许多抑制剂对CDK4/6具有良好的激酶抑制作用,在抗肿瘤方面也显示出巨大的发展潜力。然而,目前仍迫切需要开发新型 CDK4/6 抑制剂,以解决耐药性、毒性和选择性等难题。
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A patent review of small molecule CDK4/6 inhibitors in the treatment of cancer: 2020-present.

Introduction: Cyclin-dependent protein kinase 4/6 (CDK4/6) is a class of serine/threonine protein kinases that plays a key role in the regulation of the cell cycle. CDK4/6 is highly expressed in cancers such as breast cancer, melanoma, and non-small cell lung cancer (NSCLC). Currently, a variety of CDK4/6 inhibitors have been developed, aiming to develop effective inhibitors to solve CDK4/6 resistance and toxicity.

Areas covered: This article searches patents through Espacenet and reviews the development of widely studied CDK inhibitors and FDA-approved CDK4/6 inhibitors, as well as the latest progress of patented inhibitors with good inhibitory activity against CDK4/6 from 2020 to now.

Expert opinion: CDK4/6 is highly expressed in many tumors and has become an important anti-tumor target. Among the patents from 2020 to the present, many inhibitors have good kinase inhibitory effects on CDK4/6 and also show great development potential in anti-tumor. However, there is still an urgent need to develop novel CDK4/6 inhibitors that address challenges such as drug resistance, toxicity, and selectivity.

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来源期刊
CiteScore
12.10
自引率
1.50%
发文量
50
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [print], 1744-7674 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on recent pharmaceutical patent claims, providing expert opinion the scope for future development, in the context of the scientific literature. The Editors welcome: Reviews covering recent patent claims on compounds or applications with therapeutic potential, including biotherapeutics and small-molecule agents with specific molecular targets; and patenting trends in a particular therapeutic area Patent Evaluations examining the aims and chemical and biological claims of individual patents Perspectives on issues relating to intellectual property The audience consists of scientists, managers and decision-makers in the pharmaceutical industry and others closely involved in R&D Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days.
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