Technology Bundle ID
TAB-3576

Small Molecule Inhibitors of the p53/S100B Interaction for Treating Cancer

Applications
Linked ID
E-009-2017-0
Lead Inventors
Stephen Kales (NCATS)
Co-Inventors
Ajit Jadhav (NCATS)
Anton Simeonov (NCATS)
Daniel Jansen (NCATS)
David Maloney (NCATS)
Diane Luci (NCATS)
Hongmao Sun (NCATS)
ICs
This technology includes newly identified best-in-class inhibitors of the p53-S100B interaction that plays a role in malignant melanoma. S100B contributes to cancer cell proliferation (particularly malignant melanoma) by binding to p53 and inhibiting its tumor suppressor function. A high-throughput screen was used to find p53-S100B inhibitors, leading to the identification of a putative inhibitor, which was then subjected to medicinal chemistry optimization. Structure-based design was then used to develop compounds with significantly improved potency.
Commercial Applications
The identified compounds can be developed into anti-cancer agents.
Competitive Advantages
The identified compounds are best-in-class inhibitors of p53/S100B protein-protein interactions.

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