蛋白激酶Ｃβ与肿瘤的关系及其抑制剂Enzastaurin的研究进展

蛋白激酶Cβ（PKCβ）是一种丝氨酸/苏氨酸蛋白激酶，是细胞内多种信号转导通路的重要成分，参与细胞周期的调控、分化、增殖、凋亡与血管形成等多种生理过程。在许多肿瘤中观察到PKCβ活性增加，如结肠癌、乳腺癌、血液系统肿瘤等，目前临床前和临床试验中研究最多的是选择性PKCβ抑制剂Enzastaurin。本文从PKCβ的结构与功能、PKCβ与肿瘤的关系及PKCβ抑制剂Enzastaurin等方面进行综述。

Role of PKCβ in the malignant tumors and Enzastaurin, a PKCβ inhibitor

Protein kinase C beta (PKCβ) is a multifunctional serine/threonine protein kinase, which plays an important role in many cell signaling pathways.  PKCβ takes part in multiple physiological processes, including regulation of the cell cycle, differentiation, proliferation, apoptosis and angiogenesis.  Increased PKCβ activity has been observed in many human cancers, such as colon, breast and haematological malignancies.  At present, Enzastaurin is mostly studied in preclinical and clinical studies, which is a selective PKCβ inhibitor.  This   review focuses on the functional properties of PKCβ, its role played in tumors and Enzastaurin.