Allosteric and Bitopic Ligands Acting at G Protein-Coupled Receptors

本项目旨在利用新的化学工具对G蛋白偶联受体（gpcr）的功能机制有更详细的了解。gpcr是最大的细胞表面信号蛋白群，负责调节许多重要的生理功能。它们是目前使用的药品中30%以上的目标。尽管它们很重要，但关于小分子对gpcr的调控仍有许多有待了解的地方。该项目旨在通过关注这些蛋白质上的新区域（称为变抗位点）来解决这一差距，探索GPCR调节的新模式，这可能提供识别途径选择剂的潜力。

This project seeks to gain a more detailed understanding of the mechanisms of the function of G protein-coupled receptors (GPCRs) using novel chemical tools. GPCRs are the largest group of cell surface signalling proteins and are responsible for the regulation of numerous vital physiological functions. They are the target of over 30 per cent of currently used pharmaceuticals. Despite their importance, much remains to be learned about the regulation of GPCRs by small molecules. This project aims to address this gap by focusing on novel regions on these proteins, termed allosteric sites, to explore novel modes of GPCR regulation which may offer the potential of identifying pathway selective agents.