CNRS, UMR-5247, Institut des Biomolécules Max Mousseron, Faculté de Pharmacie, 15 avenue Charles Flahault, F-34000 Montpellier, France.
Trends Biotechnol. 2011 Jul;29(7):314-22. doi: 10.1016/j.tibtech.2011.03.002. Epub 2011 Apr 16.
G-protein-coupled receptors (GPCRs), the largest family of integral membrane proteins, participate in the regulation of many physiological functions and are the targets of approximately 30% of currently marketed drugs. However, knowledge of the structural and molecular bases of GPCR functions remains limited owing to difficulties related to their overexpression, purification and stabilization. The development of new strategies aimed at obtaining large amounts of functional GPCRs is therefore crucial. Here, we review the most recent advances in the production and functional folding of GPCRs from Escherichia coli inclusion bodies. Major breakthroughs open exciting perspectives for structural and dynamic investigations of GPCRs. In particular, combining targeting to bacterial inclusion bodies with amphipol-assisted folding is emerging as a highly powerful strategy.
G 蛋白偶联受体（GPCRs）是最大的跨膜蛋白家族，参与调节许多生理功能，也是目前市场上约 30%药物的靶点。然而，由于其过表达、纯化和稳定化的困难，GPCR 功能的结构和分子基础的知识仍然有限。因此，开发旨在获得大量功能 GPCR 的新策略至关重要。在这里，我们综述了从大肠杆菌包涵体中生产和功能折叠 GPCR 的最新进展。重大突破为 GPCR 的结构和动力学研究开辟了令人兴奋的前景。特别是，将靶向细菌包涵体与两亲性聚合物辅助折叠相结合，正在成为一种非常强大的策略。
