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癌症治疗的进展:CDK 和 EGFR 抑制剂的综合综述。

Advances in Cancer Therapy: A Comprehensive Review of CDK and EGFR Inhibitors.

机构信息

Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus P.O. Box 7, Palestine.

出版信息

Cells. 2024 Oct 6;13(19):1656. doi: 10.3390/cells13191656.

Abstract

Protein kinases have essential responsibilities in controlling several cellular processes, and their abnormal regulation is strongly related to the development of cancer. The implementation of protein kinase inhibitors has significantly transformed cancer therapy by modifying treatment strategies. These inhibitors have received substantial FDA clearance in recent decades. Protein kinases have emerged as primary objectives for therapeutic interventions, particularly in the context of cancer treatment. At present, 69 therapeutics have been approved by the FDA that target approximately 24 protein kinases, which are specifically prescribed for the treatment of neoplastic illnesses. These novel agents specifically inhibit certain protein kinases, such as receptor protein-tyrosine kinases, protein-serine/threonine kinases, dual-specificity kinases, nonreceptor protein-tyrosine kinases, and receptor protein-tyrosine kinases. This review presents a comprehensive overview of novel targets of kinase inhibitors, with a specific focus on cyclin-dependent kinases (CDKs) and epidermal growth factor receptor (EGFR). The majority of the reviewed studies commenced with an assessment of cancer cell lines and concluded with a comprehensive biological evaluation of individual kinase targets. The reviewed articles provide detailed information on the structural features of potent anticancer agents and their specific activity, which refers to their ability to selectively inhibit cancer-promoting kinases including CDKs and EGFR. Additionally, the latest FDA-approved anticancer agents targeting these enzymes were highlighted accordingly.

摘要

蛋白激酶在控制多种细胞过程中具有重要作用,其异常调节与癌症的发展密切相关。蛋白激酶抑制剂的实施通过改变治疗策略,显著改变了癌症治疗。近几十年来,这些抑制剂已获得 FDA 的大量批准。蛋白激酶已成为治疗干预的主要目标,特别是在癌症治疗方面。目前,FDA 已批准了 69 种针对约 24 种蛋白激酶的治疗药物,专门用于治疗肿瘤疾病。这些新型药物特异性地抑制某些蛋白激酶,如受体蛋白酪氨酸激酶、蛋白丝氨酸/苏氨酸激酶、双特异性激酶、非受体蛋白酪氨酸激酶和受体蛋白酪氨酸激酶。本综述全面介绍了激酶抑制剂的新型靶点,特别关注了细胞周期蛋白依赖性激酶 (CDKs) 和表皮生长因子受体 (EGFR)。大多数综述研究从评估癌细胞系开始,最后对单个激酶靶点进行全面的生物学评估。综述文章详细介绍了强效抗癌药物的结构特征及其特定活性,即选择性抑制促进癌症的激酶(包括 CDK 和 EGFR)的能力。此外,还相应地突出了最新获得 FDA 批准的针对这些酶的抗癌药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bf9/11476325/7dccc21fbcf3/cells-13-01656-g001a.jpg

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