Ferrer-Alegre, Marc (NCATS)
Hu, Xin (NCATS)
Marugan, Juan (NCATS)
Mathews, Lesley (NCATS)
Ford, Heide (Regents of the University of Colorado)
Blevins, Melanie (University of Colorado)
Mull, Rebecca (NCATS)
The technology includes the creation of a high-throughput assay and the identification and use of small molecules that inhibit the SIX/EYA interaction as a treatment for cancer. The Eya proteins are phosphatases that form a complex and are activated by the Six family of homeobox transcription factors. The interaction of Eya and Six mediates breast cancer cell transformation, migration, invasion and metastasis. An assay was designed to screen a large collection of compounds to identify inhibitors of the SIX/EYA interaction.
The miniaturization of the assay to a high-density screening format (1536-well plates) enables screening large collections of compounds. The identified compounds are the first small compounds that apparently inhibit the SIX/EYA interaction.