研究动态
Articles below are published ahead of final publication in an issue. Please cite articles in the following format: authors, (year), title, journal, DOI.

小分子 CDK4/6 抑制剂治疗癌症的专利审查:2020 年至今。

A patent review of small molecule CDK4/6 inhibitors in the treatment of cancer: 2020-present.

发表日期:2024 Jul 16
作者: Xiaoling Huang, Shidi Xu, Lei Duan, Shan Xu, Wufu Zhu
来源: EXPERT OPINION ON THERAPEUTIC PATENTS

摘要:

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,在细胞周期的调节中发挥关键作用。 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耐药性和毒性。本文通过Espacenet检索专利,综述了广泛研究的CDK抑制剂和FDA批准的CDK4/6抑制剂的发展以及2020年至今针对CDK4/6具有良好抑制活性的专利抑制剂的最新进展。CDK4/6在多种肿瘤中高表达,已成为重要的抗肿瘤靶点。 2020年至今的专利中,不少抑制剂对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,仍然迫切需要开发新型 CDK4/6 抑制剂来解决耐药性、毒性和选择性等挑战。
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.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.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.