Translational Immunology Section, Office of Science and Technology, National Institute of Arthritis Musculoskeletal and Skin Diseases National Institutes of Health, Bethesda, MD, 20895, USA.
BioDrugs. 2013 Oct;27(5):431-8. doi: 10.1007/s40259-013-0040-7.
Altered production of cytokines can result in pathologies ranging from autoimmune diseases to malignancies. The Janus kinase family is a small group of receptor-associated signaling molecules that is essential to the signal cascade originating from type I and type II cytokine receptors. Inhibition of tyrosine kinase enzymatic activity using small molecules has recently become a powerful tool for treatment of several malignancies. Twenty years after the discovery of these enzymes, two inhibitors for this class of kinases have been approved for clinical use and others are currently in the final stage of development. Here we review the principles of cytokines signaling, summarize our current knowledge of the approved inhibitors, and briefly introduce some of the inhibitors that are currently under development.
细胞因子的产生发生改变可导致从自身免疫性疾病到恶性肿瘤等多种病理状态。Janus 激酶家族是一小群与受体相关的信号分子，对于源自 I 型和 II 型细胞因子受体的信号级联反应至关重要。使用小分子抑制酪氨酸激酶的酶活性最近已成为治疗多种恶性肿瘤的有效工具。在发现这些酶 20 年后，已有两种该类激酶抑制剂被批准用于临床，其他抑制剂目前正处于开发的最后阶段。本文综述了细胞因子信号转导的原理，总结了目前对已批准抑制剂的认识，并简要介绍了一些正在开发中的抑制剂。
