ArticleeLife2022
Fluorescence activation mechanism and imaging of drug permeation with new sensors for smoking-cessation ligands.
Article in eLife, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. 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, 28 citations in OpenAlex.
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- Continuous Nicotine Monitors for Personal Nicotine Pharmacokinetics: A Receptor-Aware Research Agenda.Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco · 2025Review
- Simulating early steps in nicotine dependence: Pharmacokinetics, activation, and chaperoning of nicotinic receptors.Molecular pharmacology · 2025Article
- NitrOFF: An engineered fluorescent biosensor to illuminate nitrate transport in living cells.bioRxiv : the preprint server for biology · 2025Article
- State-dependent motion of a genetically encoded fluorescent biosensor.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Ranking Single Fluorescent Protein-Based Calcium Biosensor Performance by Molecular Dynamics Simulations.Journal of chemical information and modeling · 2025Article
- Measurement of Neurotransmitters and Metabolites in Cell Culture and In Vitro Using Genetically Encoded PBP-Based Biosensors.Methods in molecular biology (Clifton, N.J.) · 2025Article
- Advanced Lung-on-a-Chip Technology: Mimicking the Complex Human Lung Microenvironment.International journal of biological sciences · 2025Article
- Unlocking opioid neuropeptide dynamics with genetically encoded biosensors.Nature neuroscience · 2024Article
- Development of a novel testis-on-a-chip that demonstrates reciprocal crosstalk between Sertoli and Leydig cells in testicular tissue.Experimental & molecular medicine · 2024Article
- Interactive computational and experimental approaches improve the sensitivity of periplasmic binding protein-based nicotine biosensors for measurements in biofluids.Protein engineering, design & selection : PEDS · 2024Article
- Interactive computational and experimental approaches improve the sensitivity of periplasmic binding protein-based nicotine biosensors for measurements in biofluids.bioRxiv : the preprint server for biology · 2024Article
- Development of Advanced Oral-on-a-Chip: Replicating the Intricate Human Oral Microenvironment.International journal of biological sciences · 2024Article
- Selective Serotonin Reuptake Inhibitors within Cells: Temporal Resolution in Cytoplasm, Endoplasmic Reticulum, and Membrane.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2023Article
- Discovery and structure of a widespread bacterial ABC transporter specific for ergothioneine.Nature communications · 2022Article
- Exploiting the molecular diversity of the synapse to investigate neuronal communication: A guide through the current toolkit.The European journal of neuroscience · 2022Review
- Genetically encoded tools for in vivo G-protein-coupled receptor agonist detection at cellular resolution.Clinical and translational medicine · 2022Review
- Fluorescence Screens for Identifying Central Nervous System-Acting Drug-Biosensor Pairs for Subcellular and Supracellular Pharmacokinetics.Bio-protocol · 2022Article
- Three Mutations Convert the Selectivity of a Protein Sensor from Nicotinic Agonists to S-Methadone for Use in Cells, Organelles, and Biofluids.Journal of the American Chemical Society · 2022Article
Corrections and comments
- Erratum issued
Authors and funding
19 authors at 5 institutions in 3 countries.
Funding
Abstract
Nicotinic partial agonists provide an accepted aid for smoking cessation and thus contribute to decreasing tobacco-related disease. Improved drugs constitute a continued area of study. However, there remains no reductionist method to examine the cellular and subcellular pharmacokinetic properties of these compounds in living cells. Here, we developed new intensity-based drug-sensing fluorescent reporters (iDrugSnFRs) for the nicotinic partial agonists dianicline, cytisine, and two cytisine derivatives - 10-fluorocytisine and 9-bromo-10-ethylcytisine. We report the first atomic-scale structures of liganded periplasmic binding protein-based biosensors, accelerating development of iDrugSnFRs and also explaining the activation mechanism. The nicotinic iDrugSnFRs detect their drug partners in solution, as well as at the plasma membrane (PM) and in the endoplasmic reticulum (ER) of cell lines and mouse hippocampal neurons. At the PM, the speed of solution changes limits the growth and decay rates of the fluorescence response in almost all cases. In contrast, we found that rates of membrane crossing differ among these nicotinic drugs by >30-fold. The new nicotinic iDrugSnFRs provide insight into the real-time pharmacokinetic properties of nicotinic agonists and provide a methodology whereby iDrugSnFRs can inform both pharmaceutical neuroscience and addiction neuroscience.
Indexed as
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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.