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Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms
Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Cell and Molecular Biology, Computational Biology and Bioinformatics. Leiden Amsterdam Ctr Drug Res, Drug Discovery & Safety, Leiden.; Univ Copenhagen, Dept Drug Design & Pharmacol, Copenhagen.ORCID iD: 0000-0002-4951-9220
PharmaCtr Bonn, Pharmaceut Inst, Pharmaceut Chem 1, Bonn.
Leiden Amsterdam Ctr Drug Res, Drug Discovery & Safety, Leiden.
Heptares Therapeut, Biopk, Broadwater Rd, Welwyn Garden City, Herts.
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2018 (English)In: TIPS - Trends in Pharmacological Sciences, ISSN 0165-6147, E-ISSN 1873-3735, Vol. 39, no 1, p. 75-89Article, review/survey (Refereed) Published
Abstract [en]

The four adenosine receptors (ARs), A(1), A(2A), A(2B), and A(3), constitute a subfamily of G protein-coupled receptors (GPCRs) with exceptional foundations for structure-based ligand design. The vast amount of mutagenesis data, accumulated in the literature since the 1990s, has been recently supplemented with structural information, currently consisting of several inactive and active structures of the A(2A) and inactive conformations of the A(1) ARs. We provide the first integrated view of the pharmacological, biochemical, and structural data available for this receptor family, by mapping onto the relevant crystal structures all site-directed mutagenesis data, curated and deposited at the GPCR database (available through http://www.gpcrdb.org). This analysis provides novel insights into ligand binding, allosteric modulation, and signaling of the AR family.

Place, publisher, year, edition, pages
2018. Vol. 39, no 1, p. 75-89
National Category
Pharmacology and Toxicology Structural Biology
Identifiers
URN: urn:nbn:se:uu:diva-347706DOI: 10.1016/j.tips.2017.11.001ISI: 000418597900006PubMedID: 29203139OAI: oai:DiVA.org:uu-347706DiVA, id: diva2:1195698
Funder
Swedish Research Council, 521-2014-2118European Regional Development Fund (ERDF)German Research Foundation (DFG), FOR2372
Available from: 2018-04-06 Created: 2018-04-06 Last updated: 2018-04-06Bibliographically approved

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Jespers, WillemGutiérrez-de-Terán, Hugo

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