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07/25/2006
Life Chemicals Inc in co-operation with Otava presents new human Janus kinase 2 (JAK 2) focused library with 2 300 compounds.

This receptor-based targeted library was created by flexible docking followed by "rescoring" algorithm.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.

24/07/2006     Back to all news     25/07/2006    


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