ReviewBiochemical pharmacology2015
New paradigms in GPCR drug discovery.
Review in Biochemical pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 64 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
64 citing papers in PubMed, 168 citations in OpenAlex.
- Efficient and specific selection of high-affinity DNA aptamers targeting μ-opioid receptor via functional extracellular vesicles.Communications biology · 2026Article
- Biased signalingActa pharmaceutica Sinica. B · 2025Review
- EnGCI: enhancing GPCR-compound interaction prediction via large molecular models and KAN network.BMC biology · 2025Article
- Covalent functionalization of G protein-coupled receptors by small molecular probes.RSC chemical biology · 2025Review
- Smad transcription factors as mediators of 7 transmembrane G protein-coupled receptor signalling.Acta pharmacologica Sinica · 2025Review
- Structural basis for lipid-mediated activation of G protein-coupled receptor GPR55.Nature communications · 2025Article
- Mitochondrial Localization and Function of Adenosine Receptors.International journal of biological sciences · 2025Article
- Collective and Coordinated Conformational Changes Determine Agonism or Antagonism at the Human Trace Amine-Associated Receptor 1.ACS omega · 2023Article
- New paradigms in purinergic receptor ligand discovery.Neuropharmacology · 2023Review
- Recent Progress of Rational Modified Nanocarriers for Cytosolic Protein Delivery.Pharmaceutics · 2023Review
- Synthetic biology-inspired cell engineering in diagnosis, treatment, and drug development.Signal transduction and targeted therapy · 2023Review
- Allosteric Modulators of Dopamine DMolecules (Basel, Switzerland) · 2022Review
- Article
- Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal Stability to the SerotoninThe Journal of membrane biology · 2022Article
- A Chemical Biological Approach to Study G Protein-Coupled Receptors: Labeling the Adenosine AACS chemical biology · 2022Article
- Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HTJournal of medicinal chemistry · 2022Article
- Phenylalanine 193 in Extracellular Loop 2 of theMolecular pharmacology · 2022Article
- Disrupting GPCR Complexes with Smart Drug-like Peptides.Pharmaceutics · 2022Review
- Cholesterol-dependent endocytosis of GPCRs: implications in pathophysiology and therapeutics.Biophysical reviews · 2021Review
- Conformational plasticity and dynamic interactions of the N-terminal domain of the chemokine receptor CXCR1.PLoS computational biology · 2021Article
4 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
1 author at 1 institution in 1 country.
Funding
Abstract
G protein-coupled receptors (GPCRs) remain a major domain of pharmaceutical discovery. The identification of GPCR lead compounds and their optimization are now structure-based, thanks to advances in X-ray crystallography, molecular modeling, protein engineering and biophysical techniques. In silico screening provides useful hit molecules. New pharmacological approaches to tuning the pleotropic action of GPCRs include: allosteric modulators, biased ligands, GPCR heterodimer-targeted compounds, manipulation of polypharmacology, receptor antibodies and tailoring of drug molecules to fit GPCR pharmacogenomics. Measurements of kinetics and drug efficacy are factors influencing clinical success. With the exception of inhibitors of GPCR kinases, targeting of intracellular GPCR signaling or receptor cycling for therapeutic purposes remains a futuristic concept. New assay approaches are more efficient and multidimensional: cell-based, label-free, fluorescence-based assays, and biosensors. Tailoring GPCR drugs to a patient's genetic background is now being considered. Chemoinformatic tools can predict ADME-tox properties. New imaging technology visualizes drug action in vivo. Thus, there is reason to be optimistic that new technology for GPCR ligand discovery will help reverse the current narrowing of the pharmaceutical pipeline.
Indexed as
Identifiers
What Socratic 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 Socratic graph.