题  目：Novel Drugs and Targets for a Selective Treatment of Cancer
报告人：Lutz F. Tietze（德国化学会前主席）
        Georg-August-University Göttingen, Tammannstr. 2
        D-37077 Göttingen, Germany
时  间：2016年6月27号（星期一）上午10：30
地  点：南大仙林校区化学化工学院蒋雯若报告厅 （H201）
邀请人：强琚莉 副教授，王乐勇 教授
E-mail: ltietze@gwdg.de

Abstract：Anticancer therapy is hampered by an insufficient differentiation of normal and malignant cells by the known antiproliferant agents, resulting in severe side effects. Tumour-selective chemotherapy must therefore be based on the exploitation of phenotypic or genetic differences of malignant and normal cells. In the Antibody Directed Enzyme Prodrug Therapy (ADEPT) a non-toxic prodrug of a highly cytotoxic drug and a monoclonal antibody-enzyme conjugate are used to allow a selective liberation of the drug from the prodrug in the cancer tissue. We have recently developed novel glycosidic prodrugs 2 based on the natural antibiotic duocarmycin 1, which are up to almost one million times less cytotoxic than the prodrugs 2 in the presence of galactosidase. The IC50-values of the formed drugs 3 are as low as 150 fM. The mode of action of these compounds could be elucidated using mass spectrometry, CD-spectroscopy and X-ray crystal structure analysis. They do not attack DNA as found for 1 but aldehyde dehydrogenase as a new target in cancer therapy.