ReviewTrends in pharmacological sciences2005
Techniques: Recent developments in computer-aided engineering of GPCR ligands using the human adenosine A3 receptor as an example.
Review in Trends in pharmacological sciences, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
18 citing papers in PubMed, 65 citations in OpenAlex.
- Identification of a Different Agonist-Binding Site and Activation Mechanism of the Human P2YScientific reports · 2017Article
- Anticancer effect of adenosine on gastric cancer via diverse signaling pathways.World journal of gastroenterology · 2015Review
- Comprehensive RNA-Seq expression analysis of sensory ganglia with a focus on ion channels and GPCRs in Trigeminal ganglia.PloS one · 2013Article
- Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility.Journal of medicinal chemistry · 2011Article
- Synthesis and pharmacological characterization of a new series of 5,7-disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives as adenosine receptor antagonists: A preliminary inspection of ligand-receptor recognition process.Bioorganic & medicinal chemistry · 2010Article
- Modeling G Protein-Coupled Receptors: a Concrete Possibility.Chimica oggi · 2010Article
- Ligand and structure-based methodologies for the prediction of the activity of G protein-coupled receptor ligands.Journal of computer-aided molecular design · 2009Article
- 14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.Bioorganic & medicinal chemistry letters · 2009Article
- Comparative docking study of anibamine as the first natural product CCR5 antagonist in CCR5 homology models.Journal of chemical information and modeling · 2009Article
- Unraveling the structure and function of G protein-coupled receptors through NMR spectroscopy.Current pharmaceutical design · 2009Review
- Computational studies of the binding modes of A 2A adenosine receptor antagonists.Amino acids · 2008Article
- On the applicability of GPCR homology models to computer-aided drug discovery: a comparison between in silico and crystal structures of the beta2-adrenergic receptor.Journal of medicinal chemistry · 2008Article
- Pyrazolo-triazolo-pyrimidines as adenosine receptor antagonists: Effect of the N-5 bond type on the affinity and selectivity at the four adenosine receptor subtypes.Purinergic signalling · 2008Article
- Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition.Journal of medicinal chemistry · 2007Article
- Possible dynamic anchor points in a benzoxazinone derivative-human oxytocin receptor system--a molecular docking and dynamics calculation.Journal of molecular modeling · 2007Article
- Molecular modelling study of 2-phenylethynyladenosine (PEAdo) derivatives as highly selective A₃ adenosine receptor ligands.Purinergic signalling · 2006Article
- Progress in the pursuit of therapeutic adenosine receptor antagonists.Medicinal research reviews · 2006Review
- Purine receptors: GPCR structure and agonist design.Molecular interventions · 2004Article
Corrections and comments
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Authors and funding
3 authors at 3 institutions in 2 countries.
Funding
Abstract
G-protein-coupled receptors (GPCRs) represent the largest known family of signal-transducing molecules, and convey signals for light and many extracellular regulatory molecules. GPCRs are dysfunctional or dysregulated in several human diseases and are estimated to be the targets of >40% of the drugs used in clinical medicine today. The crystal structure of rhodopsin provides the first information on the three-dimensional structure of GPCRs, which now supports homology modeling studies and structure-based drug-design approaches. In this article, we review recent work on adenosine receptors, a family of GPCRs, and, in particular, on adenosine A(3) receptor antagonists. We focus on an iterative, bi-directional approach in which models are used to generate hypotheses that are tested by experimentation; the experimental findings are, in turn, used to refine the model. The success of this approach is due to the synergistic interaction between theory and experimentation.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.