Technology Bundle ID
TAB-3557

Inhibitors of 3-phosphoglycerate Dehydrogenase as an Anticancer Therapy

Applications
Linked ID
E-282-2014-0
Lead Inventors
Matthew Boxer (NCATS)
Co-Inventors
David Sabatini (Whitehead Institute for Biomedical Research)
Jason Rohde (NCATS)
Kyle Brimacombe (NCATS)
Michael Pacold (Whitehead Institute for Biomedical Research)
Min Shen (NCATS)
ICs
This technology includes a family of inhibitors of 3-phosphoglycerate dehydrogenase (PHGDH) which could be utilized as a treatment for cancer. These compounds are based on a carbiothioamide core and represent the first chemotype capable of inhibiting this enzyme. The compounds have in vitro IC50s of 1-5 uM and exhibit selective cytotoxicity towards PHGDH-overexpressing cell lines of ~10 uM. They exhibit at least an order of magnitude lower toxicity towards cell lines that do not express PHGDH. These compounds block flux through the serine synthesis pathway in PHGDH-overexpressing cells, and preliminarily appear to do the same in mice.
Commercial Applications
Utilization as an anticancer therapy.
Competitive Advantages
First chemotype capable of inhibiting 3-phosphoglycerate dehydrogenase.

Request More Info

Licensing Contact: