Are GPCRs Still a Source of New Targets?

• Published in: Journal of biomolecular screening Vol. 18; no. 9; pp. 947 - 966
• Main Author: Garland, Stephen L.
• Format: Journal Article
• Language: English
• Published: United States 01.10.2013
• Subjects: Anilides - chemical synthesis; Anilides - chemistry; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Binding Sites; Crystallography, X-Ray; Databases, Chemical; Drug Design; Fingolimod Hydrochloride; Humans; Immunosuppressive Agents - chemical synthesis; Immunosuppressive Agents - chemistry; Immunosuppressive Agents - pharmacology; Ligands; Propylene Glycols - chemical synthesis; Propylene Glycols - chemistry; Propylene Glycols - pharmacology; Protein Binding; Pyridines - chemical synthesis; Pyridines - chemistry; Receptors, G-Protein-Coupled - agonists; Receptors, G-Protein-Coupled - antagonists & inhibitors; Receptors, G-Protein-Coupled - chemistry; Sphingosine - analogs & derivatives; Sphingosine - chemical synthesis; Sphingosine - chemistry; Sphingosine - pharmacology; lead discovery; chemogenomics; review; functional selectivity

G-protein-coupled receptors (GPCRs) still offer enormous scope for new therapeutic targets. Currently marketed agents are dominated by those with activity at aminergic receptors and yet they account for only ~10% of the family. Progress up until now with other subfamilies, notably orphans, Family A/...