Targeting Ligand Dependent and Ligand Independent Androgen Receptor Signaling in Prostate Cancer.

摘要

We continue to make significant progress in our work with peptidomimetics targeting ligand-dependent and ligand-independent androgen receptor signaling in Prostate Cancer. We have further designed, created, tested and validated over a hundred analogues of our lead compound. We have overcome problems with solubility, off-target effects, toxicity and formulation. We have improved potency of our lead compounds, made some of them more selective for the interaction between the Androgen receptor and select coactivators and are now in the process of optimizing these compounds prior to testing in animal experiments.