Kontzias Apostolos, Laurence Arian, Gadina Massimo, O'Shea John J
F1000 Med Rep. 2012;4:5. doi: 10.3410/M4-5. Epub 2012 Mar 1.
Protein kinases are fundamental components of diverse signaling pathways, including immune cells. Their essential functions have made them effective therapeutic targets. Initially, the expectation was that a high degree of selectivity would be critical; however, with time, the use of "multikinase" inhibitors has expanded. Moreover, the spectrum of diseases in which kinase inhibitors are used has also expanded to include not only malignancies but also immune-mediated diseases. At present, thirteen kinase inhibitors have been approved in the United States, all for oncologic indications. However, there are a growing number of molecules, including several Janus kinase inhibitors, that are being tested in clinical trials for autoimmune diseases such as rheumatoid arthritis, psoriasis and inflammatory bowel diseases. It appears likely that this new class of immunomodulatory drugs will have a major impact on the treatment of immune-mediated diseases in the near future.
蛋白激酶是包括免疫细胞在内的多种信号通路的基本组成部分。它们的重要功能使其成为有效的治疗靶点。最初，人们期望高度的选择性至关重要；然而，随着时间的推移，“多激酶”抑制剂的使用范围不断扩大。此外，激酶抑制剂的应用疾病谱也已扩大，不仅包括恶性肿瘤，还包括免疫介导的疾病。目前，美国已批准了13种激酶抑制剂，均用于肿瘤适应症。然而，越来越多的分子，包括几种Janus激酶抑制剂，正在类风湿性关节炎、银屑病和炎症性肠病等自身免疫性疾病的临床试验中进行测试。这类新型免疫调节药物似乎很可能在不久的将来对免疫介导疾病的治疗产生重大影响。
