学术讲座：结合分子模拟与嗜菌体呈现技术来开发降胆固醇之peptide药物

讲座题目：结合分子模拟与嗜菌体呈现技术来开发降胆固醇之peptide药物

讲题摘要：Many studies have demonstrated the role of elevated levels of serum cholesterol in the progression of atherosclerosis and coronary heart disease. Various drugs targeting the key enzymes involved in the cholesterol biosynthesis pathway have been investigated for the treatment of hypercholesterolemia. Human squalene synthase converting farnesyl pyrophosphate to squalene, is the first committed step in sterol synthesis, making it an attractive target for therapeutic intervention. We used the recombinant human squalene synthase as the target for screening the peptide inhibitors from phage-displayed random peptide libraries. The tightly bound phages and their derived peptides were further evaluated based on their potential binding capabilities, molecular modeling characteristics and predicted ADMET properties. Several hexa-peptides and tetra-peptides were finally synthesized to assay their inhibitory effects upon human squalene synthase. The study also demonstrated an efficient way to find bioactive peptides through combining molecular modeling and phage display techniques.

主讲人：宣大卫教授

主讲人简介：

宣大卫教授为美国纽约州立大学（石溪校区）生物化学博士，专研于生物化学、分子生物、生物信息及疫苗科技，在“探索新颖抗生素”(Discovering novel antibacterial agents through targeting bacterial phosphotransfer system)及“自天然物中开发降胆固醇药物”(Exploration of inhibitors of human squalene synthase as potential drug candidates against hypercholesterolemia)两大方向有新颖发现。发表超过40余篇SCI文章。曾任台湾中山大学与东华大学生命科学系暨生物技术所教授。

宣大卫教授除专精于中草药的作用机理外，也利用计算机设计开发靶向新药。目前，已验证了自中草药及天然物分子数据库中，用计算机虚拟筛选新药的可行性，并建立了自中草药成份中，发掘新药的方法。

宣大卫教授近日与台湾“鸿海集团”接触合作，考虑后续化学分离及药物合成在大陆进行，以开创领先世界的华人生技新药产业，同时也为中国大陆相关机构分享来自中草药及天然物分子数据库中，用计算机虚拟筛选新药的心得与成果。

时间：2015年5月4日，星期一，上午10:30

地点：厦门大学药学院4楼学术报告厅