PBITE-1 is a small molecule that selectively binds ERG N-terminal Pointed (PNT) domain with Kd of 264 uM in BLI assays, directly engages ERG, selectively inhibits proliferation and invasion, and induces apoptosis in ERG-driven prostate and hematologic malignancies.
PBITE-1 selectively inhibits proliferation in all ERG+ prostate cancer and leukemia cell lines, whereas ERG- cell lines remains largely unaffected.
PBITE-1 inhibits ERG-mediated oncogenic activities.
PBITE-1 potently suppresses VCaP viability with an IC50 of 80.1 µM, whereas enzalutamide and bicalutamide shows minimal effects.
PBITE-1 suppresses growth of ERG-positive organoids, selectively suppresses the growth and survival of ERG-driven prostate cancer organoids across both mouse and human systems.
PBITE-1 treatment induces cellular apoptosis in VCaP xenograft models, through suppression of ERG-dependent transcriptional programs and induction of tumor-selective apoptosis.