Technology Bundle ID

Inhibitors of 3-phosphoglycerate Dehydrogenase as an Anticancer Therapy

Linked ID
Lead Inventors
Matthew Boxer (NCATS)
David Sabatini (Whitehead Institute for Biomedical Research)
Jason Rohde (NCATS)
Kyle Brimacombe (NCATS)
Michael Pacold (Whitehead Institute for Biomedical Research)
Min Shen (NCATS)
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.

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