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迈向将选择性酪氨酸激酶2(TYK2)抑制剂作为治疗炎症性疾病的治疗药物。

Toward selective TYK2 inhibitors as therapeutic agents for the treatment of inflammatory diseases.

作者信息

Menet Christel J

出版信息

Pharm Pat Anal. 2014 Jul;3(4):449-66. doi: 10.4155/ppa.14.23.

Abstract

The family of JAK comprises four members and has received significant attention in recent years from the pharmaceutical industry as a therapeutic target. The role of JAK is central to cytokine signaling pathways. It is believed that selective modulation of one specific JAK can lead to the inhibition of a restricted set of cytokines, which should avoid undesired side effects and get closer to the profile of biologic therapies. Consequently, selective JAK inhibition has become a major focus area of drug discovery research. A review of the TYK2 patents indicates that industry attention has recently turned toward the development of specific inhibitors. Importantly, despite the increasing number of published patents, none of these drugs have yet made it to the clinical trials.

摘要

JAK家族由四个成员组成,近年来作为治疗靶点受到了制药行业的极大关注。JAK在细胞因子信号通路中起着核心作用。据信,对一种特定JAK的选择性调节可导致对一组受限细胞因子的抑制,这应能避免不良副作用并更接近生物疗法的特点。因此,选择性JAK抑制已成为药物发现研究的一个主要重点领域。对TYK2专利的审查表明,行业关注最近已转向特定抑制剂的开发。重要的是,尽管已发表的专利数量不断增加,但这些药物中尚无一种进入临床试验阶段。

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