Recombinant GPCR expression supports various needs in drug discovery. Over-expressed receptors can be applied for binding assays to screen chemical libraries as a means of finding hits and improving affinity and selectivity of synthesized compounds. Another application is to provide overexpressed GPCRs for structural characterization as the basis of structure-based drug design. All potential expression systems have been evaluated for GPCRs with mixed results. These include cell-free Escherichia coli-based translation systems, prokaryotic expression in E. coli and Halobacterium salinarum, and eukaryotic expression in yeast, insect and mammalian cells. Several GPCRs have been expressed at relatively high levels, in the range of 1 to 10 mg/L culture. Material from large-scale receptor production has been subjected to purification attempts and further structural biology characterization.
Was this article helpful?