PKCθ小分子抑制剂及其免疫抑制作用的研究进展

Research Progresses of Small-molecule PKCθ Inhibitors and Their Immunosuppressive Effects

关键词:  PKCθ  T细胞  免疫抑制剂  小分子化合物  自身免疫性疾病

Key words:  PKCθ  T cells  immunosuppressant  small-molecule compound  autoimmune disease

摘要:

PKCθ主要大量分布在T细胞中，参与T细胞的激活，还对效应T细胞和调节性T细胞的分化和功能分别呈现促进和抑制的双向调节作用，因此被认为是新型选择性免疫抑制剂的理想作用靶点。目前已获得了多种化学结构类型的小分子PKCθ抑制剂。本文通过查阅中外文献、专利和临床试验等数据库，主要对临床试验的、合成的和天然产物来源的PKCθ小分子抑制剂及其免疫抑制作用进行了综述，并对存在的问题进行了探讨。未来的几年里，PKCθ抑制剂很可能作为新一代免疫抑制剂，为免疫性疾病患者带来福音。

Abstract:

PKCθ, which is expressed predominantly in T cells, it is required for the activation of T cells. PKCθ also positively and negatively regulate effector and regulatory T cells' differentiation and function, respectively. These attributes of PKCθ make it an attractive target for novel selective immunosuppressant. To date, there has been reported several chemical types of small-molecule PKCθ inhibitors. Herein, these synthetic or natural PKCθ inhibitors or those in clinical trial phase are reviewed, and discussed the problems needed to be solved in the development of PKCθ inhibitors. In the coming years, PKCθ inhibitors may be served as new generation of immunosuppressant and benefit patients with immunological disease.