Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms.
Trends Pharmacol Sci
; 39(1): 75-89, 2018 01.
Article
in En
| MEDLINE
| ID: mdl-29203139
ABSTRACT
The four adenosine receptors (ARs), A1, A2A, A2B, and A3, 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 A2A and inactive conformations of the A1 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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Signal Transduction
/
Receptors, Purinergic P1
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Purinergic P1 Receptor Agonists
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Purinergic P1 Receptor Antagonists
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Mutation
Limits:
Animals
/
Humans
Language:
En
Journal:
Trends Pharmacol Sci
Year:
2018
Document type:
Article