Janus Kinase 2 (Jak2)
 Janus Kinase 2 (Jak2) focused library
Ligand in Jak2 active site. Docking example from OTAVAchemicals/Life Chemicals Janus Kinase 2 (Jak2) focused library.
The detection of H-bonds between ligand and key Jak2 residue (Leu932) was used for the library preparation.


In humans, the Janus protein tyrosine kinase family (JAKs) contains four members: JAK1, JAK2, JAK3 and TYK2. JAKs phosphorylate signal transducers and activators of transcription (STATs) simultaneously with other phosphorylations required for activation, and there are several cellular mechanisms in place to inhibit JAK/STAT signaling. That one might be able to modulate selected JAK/STAT-mediated cellular signals by inhibiting JAK kinase activity to effect a positive therapeutic outcome is a tantalizing prospect, as yet incompletely realized. While current data suggest no therapeutic use for JAK1 and TYK2 inhibition, JAK2 inhibition seems a promising but not definitively tested mechanism for treatment of leukemia.


The focused libraries, including docking scores and drug-like properties, are available on request.

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Thompson JE. JAK protein kinase inhibitors.
Drug News Perspect. 2005 Jun;18(5):305-10.



 
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