title: SETting OP449 into the PP2A-activating drug family.
abstract: The protein phosphatase 2A (PP2A) tumor suppressor is inactivated in different leukemias through the activity of its endogenous inhibitors (e.g., SET), which are aberrantly regulated by oncogenic tyrosine kinases. Like other effective and nontoxic PP2A-activating drugs (PAD), OP449 inhibits SET and impairs leukemogenesis. This further supports the immediate use of PADs in patients with leukemia.
authors.affiliation: Authors' Affiliations: The Ohio State University Comprehensive Cancer Center, Columbus, Ohio; and Department of Medicine, The Greenebaum Cancer Center, University of Maryland School of Medicine, Baltimore, Maryland.
authors.forename: Paolo
authors.initials: P
authors.lastname: Neviani
authors.forename: Danilo
authors.initials: D
authors.lastname: Perrotti
mesh_terms: D000818:Animals; D004268:DNA-Binding Proteins; D019008:Drug Resistance, Neoplasm / Q000187:drug effects*; D056488:Histone Chaperones / Q000037:antagonists & inhibitors*; D006801:Humans; D007951:Leukemia, Myeloid / Q000188:drug therapy*; D008297:Male; D010455:Peptides / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D014157:Transcription Factors / Q000037:antagonists & inhibitors*
chemical_list: D004268:DNA-Binding Proteins; D056488:Histone Chaperones; C583613:OP449 peptide; D010455:Peptides; D047428:Protein Kinase Inhibitors; C513473:SET protein, human; D014157:Transcription Factors