Receptor interacting protein kinase-2 (RIPK2) is an adaptor tyrosine kinase mediating proinflammatory signaling downstream from NOD1/2 receptors. This signaling pathway has been linked to multiple diseases including inflammatory bowel disease (IBD) and multiple sclerosis (MS). Our researchers have developed compounds that are based on a new scaffold that specifically targets RIPK2 kinase activity. The compounds potently inhibits the enzyme and blocks NOD2 signaling in cells at low nanomolar concentrations.
Inflammatory Bowel disease
Blau Syndrome (early-onset sarcoidosis)
Potentially other granulomatous inflammatory conditions involving NOD signaling including adult onset sarcoidosis, and additional forms of arthritis and uveitis.
There is an urgent need for specific small molecule inhibitors of RIPK2 that can be advanced for the treatment of various inflammatory diseases with higher efficacy and minimum side-effects.
Currently, there are no FDA approved RIPK2 inhibitors.
Inhibitors of RIPK2 activity in vitro with a known mode of binding