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Novel Inhibitors of RIPK2

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.

Applications

  • Inflammatory Bowel disease
  • Multiple Sclerosis
  • Blau Syndrome (early-onset sarcoidosis)
  • Potentially other granulomatous inflammatory conditions involving NOD signaling including adult onset sarcoidosis, and additional forms of arthritis and uveitis.

Problems Addressed

  • 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.

Competitive Advantages

  • Inhibitors of RIPK2 activity in vitro with a known mode of binding
  • High specificity to RIPK2
  • Demonstrated potent activity in cell based models

Patents

  • PCT/US18/32631