Technology Bundle ID

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

Linked ID
Lead Inventors
Stephen Kales (NCATS)
Ajit Jadhav (NCATS)
Anton Simeonov (NCATS)
Daniel Jansen (NCATS)
David Maloney (NCATS)
Diane Luci (NCATS)
Hongmao Sun (NCATS)
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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