Department of Electrophysiological Diagnosis, 3201 Hospital of Xi'an Jiaotong University Health Science Center, Hanzhong 723000, China.
College of Chemical & Environment Science, Shaanxi University of Technology, Hanzhong 723001, China; Department of Stomatology, Shenzhen Second People's Hospital, Shenzhen 518035, China.
Bioorg Med Chem. 2024 Sep 1;111:117870. doi: 10.1016/j.bmc.2024.117870. Epub 2024 Aug 8.
The dysregulation of kinases has emerged as a major class of targets for anticancer drug discovery given its node roles in the etiology of tumorigenesis, progression, invasion, and metastasis of malignancies, which is validated by the FDA approval of 28 small molecule kinase inhibitor (SMKI) drugs for cancer treatment at the end of 2015. While the preclinical and clinical data of these drugs are widely presented, it is highly essential to give an updated review on the medical indications, design principles and binding modes of these anti-tumor SMKIs approved by the FDA to offer insights for the future development of SMKIs with specific efficacy and safety.
鉴于激酶的失调在肿瘤发生、发展、侵袭和转移的病因学中起着节点作用，它已成为抗癌药物发现的主要靶点之一，这一事实已被 2015 年底 FDA 批准的 28 种用于癌症治疗的小分子激酶抑制剂 (SMKI) 药物所证实。虽然这些药物的临床前和临床数据已经广泛呈现，但非常有必要对这些经 FDA 批准的抗肿瘤 SMKI 的医学适应证、设计原则和结合模式进行更新综述，为具有特定疗效和安全性的 SMKI 的未来发展提供见解。
