ArticleBioconjugate chemistry2014
Photomodulation of G protein-coupled adenosine receptors by a novel light-switchable ligand.
Article in Bioconjugate chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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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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Who cites it
22 citing papers in PubMed, 51 citations in OpenAlex.
- Ideal efficacy photoswitching for chromocontrol of TRPC4/5 channel functions in live tissues.Nature chemical biology · 2026Article
- In search of a photoswitchable drug for serotonin receptors: a molecular dynamics simulation study.RSC advances · 2025Article
- Photoswitchable positive allosteric modulators of metabotropic glutamate receptor 4 to improve selectivity.iScience · 2024Article
- Current Status and Future Strategies for Advancing Functional Circuit MappingThe Journal of neuroscience : the official journal of the Society for Neuroscience · 2023Article
- Optical Approaches for Investigating Neuromodulation and G Protein-Coupled Receptor Signaling.Pharmacological reviews · 2023Review
- Optical control of neuronal activities with photoswitchable nanovesicles.Nano research · 2023Article
- A Chemical Biological Approach to Study G Protein-Coupled Receptors: Labeling the Adenosine AACS chemical biology · 2022Article
- Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues.iScience · 2022Article
- Photoswitchable Serotonins for Optical Control of the 5-HTAngewandte Chemie (International ed. in English) · 2022Article
- Optical Control of Adenosine-Mediated Pain Modulation.Bioconjugate chemistry · 2021Article
- Optical control of purinergic signaling.Purinergic signalling · 2021Review
- Selective Photoswitchable Allosteric Agonist of a G Protein-Coupled Receptor.Journal of the American Chemical Society · 2021Article
- Mechanistic Insights into Light-Driven Allosteric Control of GPCR Biological Activity.ACS pharmacology & translational science · 2020Article
- Light-Sensitive Membrane Proteins as Tools to Generate Precision Treatments.The Journal of membrane biology · 2020Article
- Optical control of neuronal ion channels and receptors.Nature reviews. Neuroscience · 2019Review
- Reversible silencing of endogenous receptors in intact brain tissue using 2-photon pharmacology.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- A toolbox of molecular photoswitches to modulate the CXCR3 chemokine receptor with light.Beilstein journal of organic chemistry · 2019Article
- Remote control of movement disorders using a photoactive adenosine AJournal of controlled release : official journal of the Controlled Release Society · 2018Article
- Synthesis and Characterization of a Bidirectional Photoswitchable Antagonist Toolbox for Real-Time GPCR Photopharmacology.Journal of the American Chemical Society · 2018Article
- Dynamic modulation of inflammatory pain-related affective and sensory symptoms by optical control of amygdala metabotropic glutamate receptor 4.Molecular psychiatry · 2018Article
Corrections and comments
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Authors and funding
10 authors at 6 institutions in 2 countries.
Funding
Abstract
The adenosinergic system operates through G protein-coupled adenosine receptors, which have become promising therapeutic targets for a wide range of pathological conditions. However, the ubiquity of adenosine receptors and the eventual lack of selectivity of adenosine-based drugs have frequently diminished their therapeutic potential. Accordingly, here we aimed to develop a new generation of light-switchable adenosine receptor ligands that change their intrinsic activity upon irradiation, thus allowing the spatiotemporal control of receptor functioning (i.e., receptor activation/inactivation dependent on location and timing). Therefore, we synthesized an orthosteric, photoisomerizable, and nonselective adenosine receptor agonist, nucleoside derivative MRS5543 containing an aryl diazo linkage on the N(6) substituent, which in the dark (relaxed isomer) behaved as a full adenosine A3 receptor (A3R) and partial adenosine A2A receptor (A2AR) agonist. Conversely, upon photoisomerization with blue light (460 nm), it remained a full A3R agonist but became an A2AR antagonist. Interestingly, molecular modeling suggested that structural differences encountered within the third extracellular loop of each receptor could modulate the intrinsic, receptor subtype-dependent, activity. Overall, the development of adenosine receptor ligands with photoswitchable activity expands the pharmacological toolbox in support of research and possibly opens new pharmacotherapeutic opportunities.
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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.