Superior Lethal Activity of Novel BRD4-Degrading Proteolysis Targeting Chimera (PROTACs) versus  BET Protein Bromodomain Inhibitor (BETi) Against Post-Myeloprofilerative Neoplasm (MPN) Secondary AML Cells

Myeloproliferative neoplasm, myelofibrosis (MPN-MF), exhibits increased JAK-STAT signaling and often progresses ( ∼15-20%) to AML (sAML). JAK inhibitor (JAK-I) ruxolitinib (Rux) or standard induction chemotherapy is only modestly active against sAML. sAML cells commonly exhibit JAK2V617F mutation, as well as mutations in TP53, TET2, ASXL1, IDH1&2, SRSF2, RUNX1, MYC, PTPN11, NRAS and SETBP1.
Source: Clinical Lymphoma, Myeloma and Leukemia - Category: Hematology Authors: Source Type: research