Ontology highlight
ABSTRACT:
SUBMITTER: Block KM
PROVIDER: S-EPMC2796602 | biostudies-literature | 2009 Dec
REPOSITORIES: biostudies-literature
Block Katherine M KM Wang Hui H Szabó Lajos Z LZ Polaske Nathan W NW Henchey Laura K LK Dubey Ramin R Kushal Swati S László Csaba F CF Makhoul Joshua J Song Zuohe Z Meuillet Emmanuelle J EJ Olenyuk Bogdan Z BZ
Journal of the American Chemical Society 20091201 50
Selective blockade of hypoxia-inducible gene expression by designed small molecules would prove valuable in suppressing tumor angiogenesis, metastasis and altered energy metabolism. We report the design, synthesis, and biological evaluation of a dimeric epidithiodiketopiperazine (ETP) small molecule transcriptional antagonist targeting the interaction of the p300/CBP coactivator with the transcription factor HIF-1alpha. Our results indicate that disrupting this interaction results in rapid downr ...[more]