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G Protein-Coupled Receptor Deorphanizations
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2013 (English)In: Annual Review of Pharmacology and Toxicology, ISSN 0362-1642, E-ISSN 1545-4304, Vol. 53, 127-146 p.Article, review/survey (Refereed) Published
Abstract [en]

G protein-coupled receptors (GPCRs) are major regulators of intercellular interactions. They initiate these actions by being activated by a wide variety of natural ligands. Historically, ligands were discovered first, but the advent of molecular biology reversed this trend. Most GPCRs are identified on the basis of their DNA sequences and thus are initially unmatched to known natural ligands. They are termed orphan GPCRs. Discovering their ligands-i.e., "deorphanizing" the GPCRs-gave birth to the field of reverse pharmacology. This review discusses the present status of GPCR deorphanization, presents a few examples of successes and surprises, and highlights difficulties encountered in these efforts.

Place, publisher, year, edition, pages
2013. Vol. 53, 127-146 p.
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Medical and Health Sciences
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URN: urn:nbn:se:uu:diva-190100DOI: 10.1146/annurev-pharmtox-010611-134548ISI: 000323040100007PubMedID: 23020293OAI: oai:DiVA.org:uu-190100DiVA: diva2:582996
Available from: 2013-01-07 Created: 2013-01-07 Last updated: 2017-12-06Bibliographically approved

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Fredriksson, RobertSchiöth, Helgi B

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