Novel Thioredoxin Inhibitors for Breast Cancer Therapy

摘要

The hypothesis tested was that the thioredoxin redox signaling system is essential for the growth of some human breast caners and that drugs inhibiting this system will block oncogenesis and cause selective growth inhibition and/or apoptosis. The specific objectives of the IDEA proposal are to generate and identify selective inhibitors of thioredoxin using target-array chemistry methodologies, in vitro assays and cell-based screening approaches. The scope of the research activity demanded that we develop semi-automated synthetic methodology. We selected lead compounds that could be optimized as candidates for clinical development, which would encompass a Clinical Translational Research (CTR) proposal. We performed preclinical pharmacokinetics and formulation studies on interested candidates.