Inhibitors for the Glutamine Transporter ASCT2

Background:

Changes in cell metabolism support rapid growth and proliferation of tumor cells, resulting in increased reliance on the metabolism of amino acids such as glutamine (i.e., ‘glutamine addiction’). ASCT2 amino acid transporters are highly upregulated in multiple cancers, where they often function in cooperation with other mechanisms to supply tumor cells with nutrients that are used as energy supply, to build biomass, or to serve as signaling molecules to enhance cell proliferation.

 Technology Overview:

 A new class of competitive inhibitors of the glutamine transporter ASCT2 have been developed by Binghamton University, researchers, demonstrating sub-micromolar affinities, significantly improving on published and available compounds. These inhibitors will be useful to block glutamine transport in rapidly growing cancer cells, as well as serve as model compounds for basic science research of ASCTs in cell biology and metabolism. 

 Advantages:

• Affinities in the lower micromolar down to the nanomolar range.
• Increased receptor specificity.

 

 Applications:

Treatment of ASCT2-overexpressing cancers, including kidney, gastrointestinal tract and liver, the female reproductive tract, the nervous system, breast, prostate, melanoma, colorectal, pancreatic, tongue, lung, and head and neck squamous cell carcinoma. Some of these compounds have been shown to penetrate the blood brain barrier, making them useful in neuroscience research.  

Licensing Status: 

Patent Pending Seeking joint development partner, company commercialization partner