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
UNLABELLED: Medulloblastoma is one of the most common malignant brain tumors of children, and 30% of medulloblastomas are driven by gain-of-function genetic lesions in the Sonic Hedgehog (SHH) signaling pathway. EYA1, a haloacid dehalogenase phosphatase and transcription factor, is critical for tumorigenesis and proliferation of SHH medulloblastoma (SHH-MB). Benzarone and benzbromarone have been identified as allosteric inhibitors of EYA proteins. Using benzarone as a point of departure, we developed a panel of 35 derivatives and tested them in SHH-MB...
March 15, 2024: Cancer Research