ABSTRACT
G protein‐coupled receptors (GPCRs) are a large family of seven‐α‐helical transmembrane receptor proteins that have emerged as important drug targets in humans. Despite their importance and abundance in the human genome, very little structural or functional information is available for most GPCRs, limiting their accessibility as drug targets for industry. The singular challenge inherent in conducting any molecular‐level biophysical and structural study of GPCRs is obtaining a pure sample of protein with native fold and function. Traditional detergent micelle purifications have proven effective for only a small subset of all GPCRs. Therefore, novel rationally designed molecules or supramolecular assemblies are needed to expand the set of GPCRs that may be purified and studied. This entry will describe the current approaches to GPCR purification, survey a number of molecules designed to improve the standard protocol, and offer a perspective to chemists in supramolecular science who have the expertise to produce innovative solutions.
