布鲁顿酪氨酸激酶及其抑制剂研究进展

Advances in Bruton’s tyrosine kinase and its inhibitors

布鲁顿酪氨酸激酶(Bruton’s tyrosine kinase, BTK)是B细胞抗原受体信号通路的关键调节因子,在多种B细胞恶性肿瘤的发生、发展中起着重要作用。BTK抑制剂是一类新型抗肿瘤药物,现已有3个BTK抑制剂获得美国FDA批准。多项大型临床试验证实,BTK抑制剂对慢性淋巴细胞白血病和套细胞淋巴瘤的疗效良好。BTK抑制剂联合其他化疗药物治疗多种实体瘤的临床研究亦已取得一定进展。本文概要介绍BTK的结构、功能及其抑制剂的临床研究进展。

Bruton’s tyrosine kinase(BTK) is a key molecule involved in multiple functions of B cells, and also plays an important role in the occurrence and development of various B cell malignancies. In the development of BTK inhibitors targeting BTK, there are currently three BTK inhibitors approved by the FDA for marketing. Several large-scale clinical trials have found that BTK inhibitors have excellent effects on chronic lymphocytic leukemia and mantle lymphoma. More progress has been also made in the trials around BTK inhibitor combined with other chemotherapeutic drugs to treat multiple solid tumors. The structure, functions and inhibitors of BTK are reviewed in this article.