Journal
TRENDS IN PHARMACOLOGICAL SCIENCES
Volume 40, Issue 6, Pages 378-387Publisher
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2019.04.001
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Funding
- National Institute of Health [HL098062, GM007752, CA121938, HL007444, CA189477, AG053568]
- Department of Defense [W81XWH-14-1-0372]
- Bristol Myers Squibb
- ASPET David Lehr award
- Padres Pedal the Cause PTC2017 award
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G protein-coupled receptors (GPCRs) are targets for similar to 35% of approved drugs but only similar to 15% of the similar to 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.
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