学术信息

澳大利亚阿德莱德大学Simon Pyke教授讲学通知

发布时间:2018-10-08浏览次数:48来源:化工与化学学院

应化工与化学学院邀请,澳大利亚阿德莱德大学Simon Pyke教授将于近日访问我校,并为我校师生带来精彩报告。报告主要介绍Simon Pyke教授关于小分子作为蛋白质-蛋白质相互作用抑制剂的相关工作,欢迎广大师生参加。

报告时间:1012日(星期五)上午9:00

报告地点:明德楼A801

报告题目:Small molecules as Protein-Protein Interaction Inhibitors

 

报告摘要:

Cells communicate with one another through a vast array of signalling networks, which are primarily mediated by protein-protein interactions.  Protein-protein interactions are defined by the physical interaction (binding) between the surfaces of a ‘receptor’ protein and its ‘ligand’ partner protein. In this sense, the descriptor ‘receptor’ is quite metaphorical: protein-protein interactions occur at protein surfaces which are often very flat, and have a large surface area – unlike a typical ‘receptor’ that generally has a well-defined three-dimensional shape to complement its target ligand.

In disease states, protein-protein interactions are often deregulated, leading to constitutively active (i.e. always turned ‘on’) signalling pathways, tending towards a disease phenotype (e.g. manifested as unrestricted cell proliferation/growth, as in cancers). For this reason, Protein-protein interactions are attractive therapeutic targets. However, these interactions have until recently been considered too difficult to target due to the large surface areas and dynamic interfaces involved in such interactions.

We have been using the Tec SH3 domain as a model system to investigate the development of small-molecule ligands that will bind to the interaction site of the native protein interaction binding partner. An overview of the design principles, synthesis and protein-ligand binding of these small molecule ligands will be presented.