ReviewFrontiers in pharmacology2014
Discovery of GPCR ligands for probing signal transduction pathways.
Review in Frontiers in pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 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.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
20 citing papers in PubMed, 36 citations in OpenAlex.
- Do GPCRs constitute the target of 30% of newly approved drugs in Germany?Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Targeting Opioid Receptors in Addiction and Drug Withdrawal: Where Are We Going?International journal of molecular sciences · 2023Review
- Specificities of Protein Homology Modeling for Allosteric Drug Design.Methods in molecular biology (Clifton, N.J.) · 2023Article
- Potent and Subtype-Selective Dopamine DJournal of medicinal chemistry · 2021Article
- Trends in application of advancing computational approaches in GPCR ligand discovery.Experimental biology and medicine (Maywood, N.J.) · 2021Review
- Molecular Modeling of Histamine Receptors-Recent Advances in Drug Discovery.Molecules (Basel, Switzerland) · 2021Review
- Orthogonal fluorescent chemogenetic reporters for multicolor imaging.Nature chemical biology · 2021Article
- Prokineticin signaling in heart-brain developmental axis: Therapeutic options for heart and brain injuries.Pharmacological research · 2020Review
- Analysis of a Protein Network Related to Copy Number Variations in Autism Spectrum Disorder.Journal of molecular neuroscience : MN · 2019Article
- Dopamine D2 Receptors Dimers: How can we Pharmacologically Target Them?Current neuropharmacology · 2018Review
- Homo- and Heterodimerization of Proteins in Cell Signaling: Inhibition and Drug Design.Advances in protein chemistry and structural biology · 2018Review
- Sphingosine-1-Phosphate Receptor-1 Promotes Environment-Mediated and Acquired Chemoresistance.Molecular cancer therapeutics · 2017Article
- Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases.Frontiers in neuroscience · 2016Review
- Immunomodulatory Effects Mediated by Dopamine.Journal of immunology research · 2016Review
- Allosteric Modulation of Chemoattractant Receptors.Frontiers in immunology · 2016Review
- Basic Pharmacological and Structural Evidence for Class A G-Protein-Coupled Receptor Heteromerization.Frontiers in pharmacology · 2016Review
- New paradigms in GPCR drug discovery.Biochemical pharmacology · 2015Review
- Applications of phototransformable fluorescent proteins for tracking the dynamics of cellular components.Photochemical & photobiological sciences : Official journal of the European Photochemistry Association and the European Society for Photobiology · 2015Review
- Activators of G protein signaling in the kidney.The Journal of pharmacology and experimental therapeutics · 2015Review
- Editorial: Monitoring endogenous GPCRs: lessons for drug design.Frontiers in pharmacology · 2015Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
G protein-coupled receptors (GPCRs) are seven integral transmembrane proteins that are the primary targets of almost 30% of approved drugs and continue to represent a major focus of pharmaceutical research. All of GPCR targeted medicines were discovered by classical medicinal chemistry approaches. After the first GPCR crystal structures were determined, the docking screens using these structures lead to discovery of more novel and potent ligands. There are over 360 pharmaceutically relevant GPCRs in the human genome and to date about only 30 of structures have been determined. For these reasons, computational techniques such as homology modeling and molecular dynamics simulations have proven their usefulness to explore the structure and function of GPCRs. Furthermore, structure-based drug design and in silico screening (High Throughput Docking) are still the most common computational procedures in GPCRs drug discovery. Moreover, ligand-based methods such as three-dimensional quantitative structure-selectivity relationships, are the ideal molecular modeling approaches to rationalize the activity of tested GPCR ligands and identify novel GPCR ligands. In this review, we discuss the most recent advances for the computational approaches to effectively guide selectivity and affinity of ligands. We also describe novel approaches in medicinal chemistry, such as the development of biased agonists, allosteric modulators, and bivalent ligands for class A GPCRs. Furthermore, we highlight some knockout mice models in discovering biased signaling selectivity.
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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.