Liu Yan, Song Hang, Zhou Yehui, Ma Xinxing, Xu Jing, Yu Zhenghong, Chen Liming
The Key Laboratory of Bio-Medical Diagnostics, Suzhou Institute of Biomedical Engineering and Technology, Chinese Academy of Sciences, Suzhou 215163, P. R. China.
Jiangsu Key Laboratory for Molecular and Medical Biotechnology, Institute of cancer, Department of biochemistry, College of Life Science, Nanjing Normal University, Nanjing 210023, P. R. China.
J Cancer. 2021 Jan 1;12(3):735-739. doi: 10.7150/jca.50899. eCollection 2021.
Protein kinase D3 (PRKD3), a serine/threonine kinase, belongs to protein kinase D family, which contains three members: PRKD1, PRKD2, and PRKD3. PRKD3 is activated by many stimuli including phorbol esters, and G-protein-coupled receptor agonists. PRKD3 promotes cancer cell proliferation, growth, migration, and invasion in various tumor types including colorectal, gastric, hepatic, prostate, and breast cancer. Accumulating data supports that PRKD3 is a promising therapeutic target for treatment of cancer. This review discusses the functions and mechanisms of PRKD3 in promoting tumorigenesis and tumor progression of various tumor types as well as the latest developments of small-molecule inhibitors selection for PRKD/PRKD3.
蛋白激酶D3(PRKD3)是一种丝氨酸/苏氨酸激酶,属于蛋白激酶D家族,该家族包含三个成员:PRKD1、PRKD2和PRKD3。PRKD3可被多种刺激激活,包括佛波酯和G蛋白偶联受体激动剂。PRKD3在包括结直肠癌、胃癌、肝癌、前列腺癌和乳腺癌在内的多种肿瘤类型中促进癌细胞增殖、生长、迁移和侵袭。越来越多的数据支持PRKD3是治疗癌症的一个有前景的治疗靶点。本文综述了PRKD3在促进各种肿瘤类型的肿瘤发生和肿瘤进展中的功能和机制,以及针对PRKD/PRKD3的小分子抑制剂筛选的最新进展。