Research from the lab of Prof. Robert Sheaff
TU100 is a novel naphthoquinone and potential chemotherapeutic agent combining a modified ring system from anthracycline anti-tumor drugs with an isoquinoline group derived from natural alkaloids with anti-proliferative activity. TU100 demonstrated efficacy against multiple panels of tissue-specific cancer cell lines, and rapidly kills cells via induction of apoptosis. Its mechanism of action involves generation of reactive oxygen species and inhibiting topoisomerases I and II, key enzymes alleviating DNA supercoils formed during DNA replicatio. TU100’s unique mechanism of action involves topoisomerase inactivation via covalent modification of cysteine thiol(s).