ArticleMethods in molecular biology (Clifton, N.J.)2011
Studying ligand efficacy at G protein-coupled receptors using FRET.
Article in Methods in molecular biology (Clifton, N.J.), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 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
12 citing papers in PubMed, 24 citations in OpenAlex.
- Inhibitory probes for spatiotemporal analysis of GαNature chemical biology · 2026Article
- Allosteric mechanism in the distinctive coupling of GProceedings of the National Academy of Sciences of the United States of America · 2025Article
- Fast-diffusing receptor collisions with slow-diffusing peptide ligand assemble the ternary parathyroid hormone-GPCR-arrestin complex.Nature communications · 2024Article
- Descriptive molecular pharmacology of the δ opioid receptor (DOR): A computational study with structural approach.PloS one · 2024Article
- Thermodynamic architecture and conformational plasticity of GPCRs.Nature communications · 2023Article
- GProceedings of the National Academy of Sciences of the United States of America · 2020Article
- PTH hypersecretion triggered by a GABANature metabolism · 2020Article
- CaProceedings of the National Academy of Sciences of the United States of America · 2019Article
- Exploring G Protein-Coupled Receptors (GPCRs) Ligand Space via Cheminformatics Approaches: Impact on Rational Drug Design.Frontiers in pharmacology · 2018Review
- Dual role of mitochondria in producing melatonin and driving GPCR signaling to block cytochrome c release.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- Uncovering caffeine's adenosine A2A receptor inverse agonism in experimental parkinsonism.ACS chemical biology · 2014Article
- Endosomal GPCR signaling turned off by negative feedback actions of PKA and v-ATPase.Nature chemical biology · 2014Article
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
Drug "ligands" that bind G protein-coupled receptors (GPCRs) can either stimulate, fully (full agonists) or partially (partial agonists), or reduce (inverse agonists) basal receptor activity, by stabilizing different receptor conformations. The term "intrinsic efficacy" was introduced as a parameter to express the ability of a ligand to activate its receptor and to differentiate the varying signaling capacity of diverse ligands when they occupy the same fraction of a single receptor. Most methods use downstream biochemical and physiological responses as proxies of "intrinsic efficacy" but cannot measure it directly at the level of the receptor. Here I describe the development of a Förster resonance energy transfer (FRET) approach that permits the rigorous measurement of the intrinsic efficacy of a ligand directly at the level of a GPCR and independent from variation in experimental conditions. This approach also allows intrinsic efficacies of ligands to be linked with the effects of receptor polymorphisms or receptor heterodimerization.
Indexed as
Identifiers
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.