用于人类疾病的 STAT 信号转导治疗调节剂。
Therapeutic modulators of STAT signalling for human diseases.
机构信息
Cancer Biology, and Natural Products and Experimental Therapeutics Programs, University of Hawaii Cancer Center, 701 Ilalo Street, Honolulu, Hawaii 96813, USA.
出版信息
Nat Rev Drug Discov. 2013 Aug;12(8):611-29. doi: 10.1038/nrd4088.
Abstract
The signal transducer and activator of transcription (STAT) proteins have important roles in biological processes. The abnormal activation of STAT signalling pathways is also implicated in many human diseases, including cancer, autoimmune diseases, rheumatoid arthritis, asthma and diabetes. Over a decade has passed since the first inhibitor of a STAT protein was reported and efforts to discover modulators of STAT signalling as therapeutics continue. This Review discusses the outcomes of the ongoing drug discovery research endeavours against STAT proteins, provides perspectives on new directions for accelerating the discovery of drug candidates, and highlights the noteworthy candidate therapeutics that have progressed to clinical trials.
摘要
信号转导子和转录激活子（STAT）蛋白在生物学过程中具有重要作用。STAT 信号通路的异常激活也与许多人类疾病有关，包括癌症、自身免疫性疾病、类风湿关节炎、哮喘和糖尿病。自第一个 STAT 蛋白抑制剂被报道以来，已经过去了十多年，人们一直在努力发现 STAT 信号调节剂作为治疗药物。本综述讨论了针对 STAT 蛋白的正在进行的药物发现研究的结果，就加速发现候选药物的新方向提供了一些看法，并强调了已进展到临床试验的有前途的候选治疗药物。
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