Uckun Fatih M
Parker Hughes Cancer Center, Roseville, Minnesota 55113, USA.
Int Rev Immunol. 2008 Jan-Apr;27(1-2):43-69. doi: 10.1080/08830180701784588.
Targeting Bruton's tyrosine kinase (BTK) with a small-molecule inhibitor may be useful in treatment of BTK-expressing malignancies because of the antiapoptotic function of BTK in cancer cells. Furthermore, BTK inhibitors also exhibit antithrombotic properties, which may be desirable in the context of the increased risk of thromboembolic complications in cancer patients. This review will focus on the role of BTK in drug resistance in cancer, thromboembolism, and various pathologic immune responses, such as graft-versus-host disease. The therapeutic potential of targeting BTK is illustrated by discussion of the biologic activity profile of the rationally designed BTK inhibitor LFM-A13.
由于布鲁顿酪氨酸激酶（BTK）在癌细胞中具有抗凋亡功能，因此用小分子抑制剂靶向BTK可能对治疗表达BTK的恶性肿瘤有用。此外，BTK抑制剂还具有抗血栓形成特性，鉴于癌症患者发生血栓栓塞并发症的风险增加，这可能是理想的。本综述将重点关注BTK在癌症耐药性、血栓形成以及各种病理性免疫反应（如移植物抗宿主病）中的作用。通过讨论合理设计的BTK抑制剂LFM-A13的生物学活性概况，阐述了靶向BTK的治疗潜力。
