Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms

Structural Mapping of Adenosine Receptor Mutations : Ligand Binding and Signaling Mechanisms

Jespers, Willem (author): Uppsala universitet,Beräkningsbiologi och bioinformatik,Leiden Amsterdam Ctr Drug Res, Drug Discovery & Safety, Leiden.; Univ Copenhagen, Dept Drug Design & Pharmacol, Copenhagen

Schiedel, Anke C. (author): PharmaCtr Bonn, Pharmaceut Inst, Pharmaceut Chem 1, Bonn

Heitman, Laura H. (author): Leiden Amsterdam Ctr Drug Res, Drug Discovery & Safety, Leiden

Cooke, Robert M. (author): Heptares Therapeut, Biopk, Broadwater Rd, Welwyn Garden City, Herts

van Westen, Gerard J. P. (author): Leiden Amsterdam Ctr Drug Res, Drug Discovery & Safety, Leiden

Gloriam, David E. (author): Univ Copenhagen, Dept Drug Design & Pharmacol, Copenhagen

Müller, Christa E. (author): PharmaCtr Bonn, Pharmaceut Inst, Pharmaceut Chem 1, Bonn

Sotelo, Eddy (author): 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

Gutiérrez-de-Terán, Hugo (author): Uppsala universitet,Beräkningsbiologi och bioinformatik

(creator_code:org_t)

Elsevier BV, 2018
2018
English.
In: TIPS - Trends in Pharmacological Sciences. - : Elsevier BV. - 0165-6147 .- 1873-3735. ; 39:1, s. 75-89

Related links:: https://scholarlypub...; show more...; https://urn.kb.se/re...; https://doi.org/10.1...; show less...

Abstract Subject headings

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.

By the author/editor: Jespers, Willem; Schiedel, Anke C ...; Heitman, Laura H ...; Cooke, Robert M.; Kleene, Lisa; van Westen, Gera ...; show more...; Gloriam, David E ...; Müller, Christa ...; Sotelo, Eddy; Gutiérrez-de-Ter ...; show less...

About the subject

MEDICAL AND HEALTH SCIENCES: MEDICAL AND HEAL ...; and Basic Medicine; and Pharmacology and ...

NATURAL SCIENCES: NATURAL SCIENCES; and Biological Scien ...; and Structural Biolo ...

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