The Use of JAK-specific inhibitors as chemical biology tools

• Published in: Methods in molecular biology (Clifton, N.J.) Vol. 967; p. 99
• Main Authors: Burns, Christopher J, Segal, David, Wilks, Andrew F
• Format: Journal Article
• Language: English
• Published: United States 2013
• Subjects: Biology - methods; Chemistry - methods; Drug Evaluation, Preclinical; Humans; Janus Kinases - antagonists & inhibitors; Protein Kinase Inhibitors - chemistry; Protein Kinase Inhibitors - pharmacology
• ISSN: 1940-6029
• DOI: 10.1007/978-1-62703-242-1_7

The JAK family of protein tyrosine kinases are now recognized as important participants in a wide range of pathologies, from cancer to inflammatory diseases. In the last decade, the drive to develop drugs targeting members of this family has begun to deliver a panel of small molecule inhibitors of JAK family members, with a range of potencies and specificities. A number of these compounds have already found widespread use as biochemical tools in the elucidation of JAK activity in specific signaling and disease processes; however, many of the first generation compounds are poorly characterized with suboptimal potencies and selectivities.Herein, we present the data for those small molecule JAK inhibitors that have been described in the peer-reviewed literature and the benefits and potential issues that may be associated with the use of these tool compounds.