PBITE-1

PBITE-1 (PNT-Binding Inhibitor of the Transcription factor ERG) is a first-in-class small molecule inhibitor designed to target the ERG transcription factor, a key oncogenic driver in approximately 50% of prostate cancers harboring the TMPRSS2:ERG gene fusion. Developed by researchers at the University of Michigan, PBITE-1 selectively binds to a previously undruggable pocket within the N-terminal Pointed (PNT) domain of ERG. By engaging this discrete, solvent-exposed surface, the molecule inhibits the proliferation and invasion of ERG-driven cancer cells and induces apoptosis. Preclinical studies have demonstrated its efficacy in ERG-positive prostate cancer organoids and hematologic malignancy models, establishing the PNT domain as a viable therapeutic target for small molecule intervention and potential targeted protein degradation strategies.

Other names

PNT-Binding Inhibitor of the Transcription factor ERG