SETting OP449 into the PP2A-activating drug family.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 24634375.
- Also identified by DOI 10.1158/1078-0432.CCR-14-0166 and PMC identifier 4286336.
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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.
Medical subject headings
- Drug Resistance, Neoplasm
- Histone Chaperones
- Leukemia, Myeloid
- Peptides
- Protein Kinase Inhibitors
- Transcription Factors