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A Benzarone Derivative Inhibits EYA to Suppress Tumor Growth in SHH Medulloblastoma
Cancer Research 2024
Grace H. Hwang, Maria F. Pazyra-Murphy, Hyuk-Soo Seo, Sirano Dhe-Paganon, Sylwia A. Stopka, Marina DiPiazza, Nizhoni Sutter, Thomas W. Gero, Alison Volkert, Lincoln Ombelets, Georgia Dittemore, Matthew G. Rees, Melissa M. Ronan, Jennifer A. Roth, Nathalie Y.R. Agar, David A. Scott, Rosalind A. Segal
This study developed 35 benzarone derivatives and identified DS-1-38 as a brain-penetrant antagonist of the EYA phosphatase that suppresses Sonic Hedgehog-driven medulloblastoma growth in vitro and in vivo and extends survival in mice. To confirm target engagement, Flow Induced Dispersion Analysis (FIDA), on a Fida 1 instrument, was used to measure the binding affinity of DS-1-38 to EYA1 by tracking the change in the protein's hydrodynamic radius via intrinsic fluorescence and fitting a 1:1 model. It is an example of using FIDA to confirm small-molecule–protein binding affinity in solution.
