GPCRomics: An Approach to Discover GPCR Drug Targets
| Autor: | Shu Z. Wiley, Matthew W. Gorr, Paul A. Insel, Amy M. Chinn, Alexander V. Michkov, Krishna Sriram, Cristina Salmerón |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Drug media_common.quotation_subject Messenger RNA-sequencing Computational biology Biology Toxicology Medical and Health Sciences Article Receptors G-Protein-Coupled 03 medical and health sciences G-Protein-Coupled 0302 clinical medicine G protein-coupled receptors Receptors Drug Discovery Humans cyclic AMP Pharmacology & Pharmacy Molecular Targeted Therapy RNA Messenger Biological sciences media_common G protein-coupled receptor Pharmacology Base Sequence Biological Sciences 030104 developmental biology Expression data gene expression Functional activity RNA cancer-associated fibroblasts 030217 neurology & neurosurgery hormones hormone substitutes and hormone antagonists G proteins |
| Zdroj: | Trends Pharmacol Sci Trends in pharmacological sciences, vol 40, iss 6 |
| ISSN: | 1873-3735 |
| Popis: | G protein-coupled receptors (GPCRs) are targets for ∼35% of approved drugs but only ∼15% of the ∼800 human GPCRs are currently such targets. GPCRomics, the use of unbiased, hypothesis-generating methods [e.g., RNA-sequencing (RNA-seq)], with tissues and cell types to identify and quantify GPCR expression, has led to the discovery of previously unrecognized GPCRs that contribute to functional responses and pathophysiology and that may be therapeutic targets. The combination of GPCR expression data with validation studies (e.g., signaling and functional activities) provides opportunities for the discovery of disease-relevant GPCR targets and therapeutics. Here, we review insights from GPCRomic approaches, gaps in knowledge, and future directions by which GPCRomics can advance GPCR biology and the discovery of new GPCR-targeted drugs. |
| Databáze: | OpenAIRE |
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