Abstract TRPV6, a calcium channel, is an oncochannel that is overexpressed in epithelial cancers, especially prostate cancer. We have observed that concomitant TRPV6 and AR inhibition is synergistic in prostate cancer cells resulting in a strong anti-proliferative effect. Our preclinical candidate QED-203 inhibits TRPV6-mediated calcium influx (FLIPR and electrophysiology) and NFAT activity (NFAT luciferase reporter) with low nM potency and potently inhibits AR (AR ligand displacement, AR lucife
Abstract 414: QED-203, a dual TRPV6 and AR small molecule preclinical candidate for advanced prostate cancer resistant to standard of care.
Kimberley A. Beaumont·Brian Dymock·Mei Yeh·Rebecca Farrow·Matthew M. W. McLachlan·Therese L. Johnson·Akanksha Upadhyaya·Aaron M. Gregson·Raphaël Rahmani·Claire Levrier·Hasanthi Wijesekera·Malika Kumasiri·Grant Stuchbury·Terrie-Anne Cock·Andrew Harvey·Gregory R. Monteith·Rebecca H. Pouwer