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Autoimmune disease

Autoimmune disease

Protein kinase Cq (PRKCQ)

Mouse and in vitro studies identified pyrazolo-[3,4-b]pyridine-based PRKCQ inhibitors that could help treat autoimmune diseases. In vitro, the lead compound inhibited PRKCQ with an IC50 value of 0.08 nM and 75-fold selectivity over related protein kinase C (PKC) isoforms. In mice, the lead compound decreased serum levels of the proinflammatory cytokine Il-2 compared with vehicle. Next steps include testing the class of inhibitors in models of autoimmune disease and evaluating their toxicity.

SciBX 6(9); doi:10.1038/scibx.2013.209
Published online March 7, 2013

Patent application filed; licensing status undisclosed

Jimenez, J.-M. et al. J. Med. Chem.; published online Feb. 11, 2013;
Contact: Juan-Miguel Jimenez, Vertex Pharmaceuticals Inc., Oxfordshire, U.K.