G Protein Coupled Receptors (GPCRs) are therapeutic targets for many medications used to treat a variety of disease states. A large number of genetic variants have been identified in the genes coding for GPCRs and functional significance of these genetic variants continues to be explored. Changes to receptor function have already been associated with many of the identified genetic variations of these receptors. The effects of these GPCR genetic variants on the interaction of these receptors with the drugs that target them is an area of interest. Some changes in GPCR response to drugs in the presence of genetic variations of the receptors have been identified, but the application of GPCR pharmacogenomics in clinical practice is not yet fully realized. This is due to the complex nature of the associations between receptor genetic variability and drug response. More data is needed to fully understand the significance of GPCR genetic variants in patient responses to medications. With more information, GPCR pharmacogenomics may eventually prove to be useful in personalizing  medication use. Some current areas of GPCR exploration include medications used in cardiovascular disease and in some psychiatric condition. The current state of pharmacogenomics application in these areas of clinical practice will be discussed.

Learning Objectives:

1. Describe how GPCR variants may affect receptor function.

2. Describe how these genetic variants may affect drug response.

3. List GPCR genetic variants that are being evaluated for their potential clinical impact.