Chang Yu, Zhang Qingwen, Li Zhengqiu, Ding Ke, Lu Xiaoyun
School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China.
State Key Laboratory of Respiratory Diseases, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, No. 190, Kaiyuan Avenue, Science Park, Guangzhou, China.
Curr Med Chem. 2016;23(33):3801-3812. doi: 10.2174/0929867323666160920104121.
Leucine-zipper and sterile-α motif kinase (ZAK) is a member of mixed-lineage kinase family (MLKs), which is considered as a new potential target for different physiological disorders, including myocardial hypertrophy and cardiac fibrosis, inflammation and cancer. However, the progress on its biological functions and small molecule inhibitors is limited. Only several multi-kinases inhibitors are reported to non-selectively bind with ZAK with various potencies. Herein, we provide an updated overview on the biological functions and small molecular inhibitors of ZAKs.
亮氨酸拉链和无菌α基序激酶(ZAK)是混合谱系激酶家族(MLKs)的成员,被认为是包括心肌肥大、心脏纤维化、炎症和癌症在内的不同生理疾病的新潜在靶点。然而,其生物学功能和小分子抑制剂的研究进展有限。仅报道了几种多激酶抑制剂能以不同效力与ZAK非选择性结合。在此,我们提供了关于ZAK生物学功能和小分子抑制剂的最新综述。