Inhibitors Of P90 Rsk

Technology Description

UNMET NEED: This invention addresses the lack of potent and selective reversible inhibitors for RSK proteins, which play a critical role in disease progression.

TECHNOLOGY: The invention introduces a new class of reversible covalent inhibitors targeting the p90 ribosomal S6 kinases (RSK1 and RSK2), a family of proteins implicated in cancer, immune/inflammation disorders, and heart disease. The lead compound demonstrates stability, cellular activity, and therapeutic potential, overcoming challenges faced by earlier-generation inhibitors.

DEVELOPMENT STAGE: The development is at the pre-clinical proof-of-concept stage, with promising pharmacokinetic data and upcoming efficacy studies.

COMPETITIVE ADVANTAGE:

• Reversible Covalent Inhibition: First rational design of reversible covalent inhibitors targeting RSK, enabling safer therapeutic profiles for chronic diseases.
• Chemical Innovation: Utilizes a unique combination of electron-withdrawing groups to achieve reversible binding to cysteine residues, a groundbreaking approach in inhibitor development.
• High Potency and Selectivity: Exhibits picomolar binding affinity and specificity for RSK1/RSK2, outperforming existing inhibitors in terms of efficacy and selectivity.

This innovative approach holds significant promise for advancing treatments in oncology, cardiology, and immunology.

Patent Status