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Adenosine receptors as therapeutic targets
Adenosine receptors are major targets of caffeine, the most commonly consumed drug in the world. There is growing evidence that they could also be promising therapeutic targets in a wide range ofExpand
Structure of an Agonist-Bound Human A2A Adenosine Receptor
Changes associated with conformationally selective agonist binding shed light on G protein–coupled receptor activation. Activation of G protein–coupled receptors upon agonist binding is a criticalExpand
Structure of the human P2Y12 receptor in complex with an antithrombotic drug
P2Y receptors (P2YRs), a family of purinergic G-protein-coupled receptors (GPCRs), are activated by extracellular nucleotides. There are a total of eight distinct functional P2YRs expressed in human,Expand
Two disparate ligand-binding sites in the human P2Y1 receptor
In response to adenosine 5′-diphosphate, the P2Y1 receptor (P2Y1R) facilitates platelet aggregation, and thus serves as an important antithrombotic drug target. Here we report the crystal structuresExpand
Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors.
The physiological role of the P2Y(6) nucleotide receptor may involve cardiovascular, immune and digestive functions based on the receptor tissue distribution, and selective antagonists for thisExpand
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
Human P2Y receptors encompass at least eight subtypes of Class A G protein-coupled receptors (GPCRs), responding to adenine and/or uracil nucleotides. Using a BLAST search against the Homo sapiensExpand
A2B adenosine receptor blockade inhibits growth of prostate cancer cells
The role of the A2B adenosine receptor (AR) in prostate cell death and growth was studied. The A2B AR gene expression quantified by real-time quantitative RT-PCR and Western blot analysis was theExpand
Structural Determinants of A3 Adenosine Receptor Activation: Nucleoside Ligands at the Agonist/Antagonist Boundary
Mutagenesis of the human A3 adenosine receptor (AR) suggested that certain amino acid residues contributed differently to ligand binding and activation processes. Here we demonstrated that variousExpand
Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.
A three-dimensional model of the human A(2A) adenosine receptor (AR) and its docked ligands was built by homology to rhodopsin and validated with site-directed mutagenesis and the synthesis ofExpand
Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.
(N)-Methanocarba nucleosides containing bicyclo[3.1.0]hexane replacement of the ribose ring previously demonstrated selectivity as A(3) adenosine receptor (AR) agonists (5'-uronamides) or antagonistsExpand