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.

CDK12 作为癌症治疗靶点和相关抑制剂的开发。

Development of CDK12 as a Cancer Therapeutic Target and Related Inhibitors.

发表日期:2024 Jul 04
作者: Biqing Chen, Jiaqi Liu
来源: Cellular & Molecular Immunology

摘要:

细胞周期蛋白依赖性激酶 12 (CDK12) 是一种细胞周期蛋白依赖性激酶 (CDK),在转录、翻译、mRNA 剪接、细胞周期调节和 DNA 损伤修复等多种生物过程中发挥着至关重要的作用。 CDK12 失调与肿瘤发生有关,并且已在多种癌症类型中发现了影响 CDK12 的基因改变,包括乳腺癌、卵巢癌、胃癌和前列腺癌。大量研究表明,抑制CDK12表达可有效抑制肿瘤生长和增殖,强调其作为癌症生物标志物和癌症治疗中潜在治疗靶点的重要性。对 CDK12 的全面理解有望显着促进癌症治疗和预防新方法的进步。近年来,人们致力于配制CDK12的靶向抑制剂,例如PROTAC和分子凝胶降解剂。与此同时,CDK12小分子抑制剂与免疫疗法联合应用作为潜在策略的研究也已展开。本文探讨了 CDK12 在基因表达调节中的多种功能及其对人类肿瘤的影响。具体来说,它探讨了最近发现的 CDK12 激酶在各种细胞过程中的作用,强调 CDK12 作为人类肿瘤管理的可行治疗靶点的潜力。此外,这篇综述提供了在肿瘤治疗中利用 CDK12 所取得的进展的最新描述。版权所有 © Bentham Science Publishers;如有任何疑问,请发送电子邮件至 epub@benthamscience.net。
Cyclin-dependent Kinase 12 (CDK12) is a Cyclin-dependent Kinase (CDK) that plays a crucial role in various biological processes, including transcription, translation, mRNA splicing, cell cycle regulation, and DNA damage repair. Dysregulation of CDK12 has been implicated in tumorigenesis, and genetic alterations affecting CDK12 have been identified in multiple cancer types, including breast cancer, ovarian cancer, gastric cancer, and prostate cancer. Numerous studies have demonstrated that suppression of CDK12 expression effectively inhibits tumor growth and proliferation, underscoring its significance as a cancer biomarker and a potential therapeutic target in cancer treatment. A thorough comprehension of CDK12 is expected to significantly enhance the advancement of novel approaches for the treatment and prevention of cancer. In recent times, endeavors have been undertaken to formulate targeted inhibitors for CDK12, such as PROTAC and molecular gel degraders. Concurrently, investigations have been conducted on the combined utilization of CDK12 small molecule inhibitors and immunotherapy as a potential strategy. This paper examines the diverse functions of CDK12 in the modulation of gene expression and its implications in human tumors. Specifically, it explores the recently uncovered roles of CDK12 kinases in various cellular processes, emphasizing the potential of CDK12 as a viable therapeutic target for the management of human tumors. Furthermore, this review provides an up-to-- date account of the advancements made in utilizing CDK12 in tumor therapy.Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.