Proteomics

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Effect of SMARCA2/SMARCA4 inhibitor, FHD-286, on protein expression alterations in cultured cell line or patient-derived AML cells with MECOM rearrangement and expression of EVI1


ABSTRACT: Patient-derived AML191 (acute myeloid leukemia with inv3(q21;q26.2)), -7) cells were treated in duplicate with 100 nM of FHD-286 for 0, 8, 16, 24 and 48 hours to determine the global protein expression alterations that correlate with the cell cycle, growth inhibitory and lethal effects of treatment with a small molecule, chromatin remodeling complex protein, dual SMARCA2/SMARCA4 enzymatic activity inhibitor in MECOM-rearranged AML cells with EVI1 overexpression.

INSTRUMENT(S):

ORGANISM(S): Homo Sapiens (human)

SUBMITTER: Antrix Jain  

LAB HEAD: Kapil N. Bhalla

PROVIDER: PXD059059 | Pride | 2026-01-23

REPOSITORIES: Pride

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Publications


In AML with 3q26.2 rearrangements (r) the distal GATA2 hematopoietic enhancer becomes aberrantly relocated leading to activation of EVI1 expression. EVI1 is a transcriptional regulator that plays a role in proliferation and maintenance of a stem cell-like phenotype in AML. BRG1 (SMARCA4) and BRM (SMARCA2) are the mutually exclusive ATPases of the BAF (BRG1/BRM-associated factor) chromatin remodeling complexes. They regulate access to enhancers/promoters and gene-expressions orchestrating AML ste  ...[more]

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