Title : Insights into kinetic mechanism of Janus kinase 3 and its inhibition by tofacitinib.

Pub. Date : 2016 Dec 15

PMID : 27555492






3 Functional Relationships(s)
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1 Insights into kinetic mechanism of Janus kinase 3 and its inhibition by tofacitinib. tofacitinib Janus kinase 3 Homo sapiens
2 The studies presented in this report were undertaken to elucidate the kinetic mechanism of the JAK3 kinase domain, investigate the role of activation loop phosphorylation in regulating its catalytic activity, and examine its inhibition by the anti-rheumatoid arthritis drug, tofacitinib. tofacitinib Janus kinase 3 Homo sapiens
3 Kinetic analysis of JAK3 inhibition by tofacitinib indicated inhibition is time dependent, characterized by on- and off-rate constants of 1.4 +- 0.1 muM-1s-1 and 0.0016 +- 0.0005 s-1, respectively. tofacitinib Janus kinase 3 Homo sapiens