The DOI matches its Crossref record; 68 of the 68 references it cites were found in a registry or an index.
Pharmacogenomics of GPCR Drug Targets
Open accessAbstract
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 Cholecystokinin-A receptors could lead to altered or adverse drug response. By analyzing UK National Health Service drug prescription and sales data, we suggest that characterizing GPCR variants could increase prescription precision, improving patients' quality of life, and relieve the economic and societal burden due to variable drug responsiveness. VIDEO ABSTRACT.
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Self-citationA comprehensive map of molecular drug targets
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Self-citationHuman gain-of-function MC4R variants show signaling bias and protect against obesity
Lotta, L. A., Mokrosiński, J., Mendes de Oliveira, E., Li, C., Sharp, S. J., Luan, J., Brouwers, B., Ayinampudi, V., Bowker, N., Kerrison, N., et al. (2019) · Cell · doi:10.1016/j.cell.2019.03.044 · Cited by 284
Melatonin in type 2 diabetes mellitus and obesity
Karamitri, A., & Jockers, R. (2019) · Nature Reviews Endocrinology · doi:10.1038/s41574-018-0130-1 · Cited by 268
Structures of the σ2 receptor enable docking for bioactive ligand discovery
Alon, A., Lyu, J., Braz, J. M., Tummino, T. A., Craik, V., O’Meara, M. J., Webb, C. M., Radchenko, D. S., Moroz, Y. S., Huang, X.-P., et al. (2021) · Nature · doi:10.1038/s41586-021-04175-x · Cited by 211
Raman-guided subcellular pharmaco-metabolomics for metastatic melanoma cells
Du, J., Su, Y., Qian, C., Yuan, D., Miao, K., Lee, D., Ng, A. H. C., Wijker, R. S., Ribas, A., Levine, R. D., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-18376-x · Cited by 171
Metadata
- Authors
- Hauser, A. S., Chavali, S., Masuho, I., Jahn, L. J., Martemyanov, K. A., Gloriam, D. E., & Babu, M. M.
- Venue
- Cell
- Publisher
- Elsevier BV
- Published
- 2018-01
- Volume
- 172
- Issue
- 1-2
- Pages
- 41-54.e19
- ISSN
- 0092-8674 (ISSN-L)
- OpenAlex
- W2774455409
- Cited by
- 616
- References
- 68
- FWCI
- 57.65
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Hauser, A. S., Chavali, S., Masuho, I., Jahn, L. J., Martemyanov, K. A., Gloriam, D. E., & Babu, M. M. (2018). Pharmacogenomics of GPCR Drug Targets. Cell. https://doi.org/10.1016/j.cell.2017.11.033
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
