In conclusion, GPCRs have long been highly desired drug discovery targets by the pharmaceutical industry, resulting in the development of many of the best-selling drugs on the market today that account for nearly 25% of total drug sales and prescriptions. Drugs targeting these receptors have a diverse variety of therapeutic indications including allergies, cancer, pain management, and diseases affecting cardiovascular, central nervous system, gastrointestinal, and metabolic functions. Developing new GPCR therapeutics begins with the selection of a receptor for a drug discovery effort that involves evaluation of a number of parameters including bioinformatic approaches, receptor localization, potential druggability, and validation as a potential drug target. Advances in GPCR research that offer future opportunities for drug discovery efforts include orphan GPCRs, of which approximately 160 await identification of their cognate ligands and serve as the foci of extensive research to determine their physiological roles. Moreover, GPCR oligomerization offers opportunities for potentially useful therapeutics. Based on their history and future potential, GPCRs should continue to be prime therapeutic targets for drug discovery efforts by the pharmaceutical industry.

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