Pharmacogenomics of GPCR Drug Targets
University of Copenhagen · MRC Laboratory of Molecular Biology · +2 more institutions
Abstract
Natural genetic variation in the human genome is a cause of individual differences in responses to medications and is an underappreciated burden on public health. Although 108 G-protein-coupled receptors (GPCRs) are the targets of 475 (∼34%) Food and Drug Administration (FDA)-approved drugs and account for a global sales volume of over 180 billion US dollars annually, the prevalence of genetic variation among GPCRs targeted by drugs is unknown. By analyzing data from 68,496 individuals, we find that GPCRs targeted by drugs show genetic variation within functional regions such as drug- and effector-binding sites in the human population. We experimentally show that certain variants of μ-opioid and…
Citation impact
- FWCI
- 25.57
- Percentile
- 100%
- References
- 70
Authors
7Topics & keywords
- Biology
- Pharmacogenomics
- G protein-coupled receptor
- Drug
- Computational biology
- Pharmacology
- Bioinformatics
- Receptor