Progress toward JAK1-selective inhibitors

被引：6

作者：

Menet, Christel J. ^{[1
]}

Mammoliti, Oscar ^{[1
]}

Lopez-Ramos, Miriam ^{[2
]}

机构：

[1] Dept Med Chem, B-2800 Mechelen, Belgium

[2] Galapagos SASU, Dept Computat Chem & Biol, F-93230 Romainville, France

来源：

FUTURE MEDICINAL CHEMISTRY | 2015年 / 7卷 / 02期

关键词：

JAK1; INHIBITORS; PROTEIN-KINASE; PRECLINICAL CHARACTERIZATION; SELECTIVITY; DISCOVERY; POTENT; TYK2; IDENTIFICATION; IMIDAZOPYRROLOPYRIDINES; PYRROLOPYRIDINES;

D O I：

10.4155/FMC.14.149

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

The discovery of the JAK-STAT pathway was a landmark in cell biology. The identification of these pathways has changed the landscape of treatment of rheumatoid arthritis and other autoimmune diseases. The two first (unselective) JAK inhibitors have recently been approved by the US FDA for the treatment of myelofibrosis and rheumatoid arthritis and many other JAK inhibitors are currently in clinical development or at the discovery stage. Research groups have demonstrated the different roles of JAK member and the therapeutic potential of targeting them selectively. JAK1 plays a critical and potentially dominant role in the transduction of gamma c cytokine (gamma c = common gamma chain) and in IL-6 signaling. In this review, we will discuss the state-of-the-art research that evokes JAK1 selective inhibition.

引用

页码：203 / 235

页数：33

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