搜索:   联系我们 |  English 


    发布时间:2016-06-23 14:00:15    点击:2255

高济宇有机化学前沿讲座


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.

地址:江苏省南京市栖霞区仙林大道163号南京大学化学楼    邮编:210023    电话:86-25-89682304   传真:86-25-89687761

© 2010-2018   南京大学 化学化工学院