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Structural Mapping ...
Structural Mapping of Adenosine Receptor Mutations : Ligand Binding and Signaling Mechanisms
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- Jespers, Willem (författare)
- Uppsala universitet,Beräkningsbiologi och bioinformatik,Leiden Amsterdam Ctr Drug Res, Drug Discovery & Safety, Leiden.; Univ Copenhagen, Dept Drug Design & Pharmacol, Copenhagen
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- Schiedel, Anke C. (författare)
- PharmaCtr Bonn, Pharmaceut Inst, Pharmaceut Chem 1, Bonn
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- Heitman, Laura H. (författare)
- Leiden Amsterdam Ctr Drug Res, Drug Discovery & Safety, Leiden
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- Cooke, Robert M. (författare)
- Heptares Therapeut, Biopk, Broadwater Rd, Welwyn Garden City, Herts
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- Kleene, Lisa (författare)
- PharmaCtr Bonn, Pharmaceut Inst, Pharmaceut 1, Bonn
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- van Westen, Gerard J. P. (författare)
- Leiden Amsterdam Ctr Drug Res, Drug Discovery & Safety, Leiden
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- Gloriam, David E. (författare)
- Univ Copenhagen, Dept Drug Design & Pharmacol, Copenhagen
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- Müller, Christa E. (författare)
- PharmaCtr Bonn, Pharmaceut Inst, Pharmaceut Chem 1, Bonn
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- Sotelo, Eddy (författare)
- Univ Santiago de Compostela, Fac Farm, Ctr Singular Invest Quim Biolox & Mat Mol CIQUS, Santiago De Compostela 15782, Spain.; Univ Santiago de Compostela, Fac Farm, Dept Quim Organ, Santiago De Compostela
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- Gutiérrez-de-Terán, Hugo (författare)
- Uppsala universitet,Beräkningsbiologi och bioinformatik
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(creator_code:org_t)
- Elsevier BV, 2018
- 2018
- Engelska.
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Ingår i: TIPS - Trends in Pharmacological Sciences. - : Elsevier BV. - 0165-6147 .- 1873-3735. ; 39:1, s. 75-89
- Relaterad länk:
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https://scholarlypub...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- 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.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
- NATURVETENSKAP -- Biologi -- Strukturbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Structural Biology (hsv//eng)
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