GPCRomics: An Approach to Discover GPCR Drug Targets

• Published in: Trends in pharmacological sciences (Regular ed.) Vol. 40; no. 6; pp. 378 - 387
• Main Authors: Insel, Paul A., Sriram, Krishna, Gorr, Matthew W., Wiley, Shu Z., Michkov, Alexander, Salmerón, Cristina, Chinn, Amy M.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.06.2019
• Subjects: Base Sequence; cancer-associated fibroblasts; cyclic AMP; Drug Discovery - methods; G protein-coupled receptors (GPCRs); G proteins; gene expression; Humans; Molecular Targeted Therapy; Receptors, G-Protein-Coupled - agonists; Receptors, G-Protein-Coupled - antagonists & inhibitors; Receptors, G-Protein-Coupled - biosynthesis; Receptors, G-Protein-Coupled - genetics; RNA, Messenger - genetics; RNA, Messenger - metabolism; RNA-sequencing; RNA-sequencing; cyclic AMP; cancer-associated fibroblasts; G protein-coupled receptors (GPCRs); G proteins; gene expression

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 expre...