Bromodomain and extra-terminal (BET) proteins are chromatin readers that preferentially affect the transcription of genes with super-enhancers, including oncogenes.
BET proteins bind acetylated histone tails via their bromodomain, bringing the elongation complex to the promoter region. OTX015 specifically binds to BRD2, BRD3 and BRD4 to prevent BET proteins from binding to chromatin, inhibiting gene transcription.
OTX015 inhibits proliferation in many haematological malignancy cell lines and patient cells, in vitro and in vivo. OTD Therapeutic Development aimed to establish the recommended dose of OTX-15 in patients with haematological malignancies.
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