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Forays in Drug Discovery

报告人: Jonathan Baell            

            Professor of Medicinal Chemistry, Monash Institute of

               Pharmaceutical Sciences (MIPS), Monash University.

 

时 间: 201874星期三 ,下午04:00

地 点化学院A717

 

Abstract:In this talk we will explore a variety of our forays in recent years into drug discovery, from antiparasitic to anticancer agents with screening, design or the literature as starting points. On one hand, we view high throughput screening (HTS) as a central science for such ambitions, so that we can find new starting points for medicinal chemistry against targets of interest. For example, we identified a screening hit from HTS that targeted a protein kinase of interest to us – LIMK1 - and for which we had genetic evidence of its relevance to metastasis. This ultimately led to an intriguing outcome – an unexpected but necessary twist in the tail. On the other hand, in a separate project, we took a compound from the literature and successfully engineered a heterocyclic isostere with potent cell-based activity that we showed was mechanism-based and acting on the pro-survival proteins Bcl-xL and Bcl-2. We also took the structure of protein ligands to Bcl-xL to design active peptidomimetics of the interfacial binding epitope. Finally, using HTS we have discovered potent antiparasitics that target Trypanosomes – the causative agents of neglected diseases such as Sleeping Sickness and Chagas’ Disease

 

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