Abstract
GPCRs (G-protein-coupled receptors) are the largest class of cell-surface receptors. They are the targets of many bio-active molecules and thus could be promising targets for drugs. However, our understanding of GPCR is restricted mainly due to the difficulties of their expression and/or purification as recombinant proteins. In this paper, our studies about chemokine receptor (CXCR1) are shown as a model case of the investigation of GPCR, and the prospects of this field of research are discussed.