Superior Lethal Activity of Novel BET Protein Proteolysis Targeting Chimera (BETP-PROTACs) Versus Betp Bromodomain Inhibitor (BETi) Against Post-Myeloproliferative Neoplasm (MPN) Secondary (s) AML Cells
Saenz D, Fiskus W, Raina K, Manshouri T, Coleman K, Winkler J, Qian Y, Crew A, Shen A, Mill C, Sun B, Verstovsek S, Crews C, Bhalla K. Superior Lethal Activity of Novel BET Protein Proteolysis Targeting Chimera (BETP-PROTACs) Versus Betp Bromodomain Inhibitor (BETi) Against Post-Myeloproliferative Neoplasm (MPN) Secondary (s) AML Cells. Blood 2016, 128: 747. DOI: 10.1182/blood.v128.22.747.747.Peer-Reviewed Original ResearchTyk2 tyrosine kinaseMPN-MFARV-825Stem/progenitor cellsHEL92.1.7 cellsHematopoietic stem/progenitor cellsProgenitor cellsC-MycP-STAT5ARV-771BETi treatmentMass cytometry approachProtein expressionLoss of responseNormal hematopoietic progenitor cellsNotable clinical benefitJAK-STATProtein array analysisNegative myeloproliferative neoplasmsBcl-xLMedian survivalClinical outcomesClinical benefitHematopoietic progenitor cellsWestern analysis