ArticleProceedings of the National Academy of Sciences of the United States of America2017
Dual optical control and mechanistic insights into photoswitchable group II and III metabotropic glutamate receptors.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
What it found
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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.
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Who cites it
42 citing papers in PubMed, 89 citations in OpenAlex.
- A Systematic Benchmark Study of Free Energy Methods for Quantifying Light-Responsive Binding Affinities of Photoswitchable Antagonists of Beta-Adrenergic Receptors.Journal of medicinal chemistry · 2026Article
- Covalent anchoring of tethered ligands to chemogenetic handles for targeted in vivo neuropharmacology.STAR protocols · 2025Article
- Reversible Antagonism of Dopamine D1 Receptor Using a Photoswitchable Remotely Tethered Ligand.ACS chemical biology · 2025Article
- Article
- Principles and Design of Molecular Tools for Sensing and Perturbing Cell Surface Receptor Activity.Chemical reviews · 2025Review
- A Simplified Guide RNA Synthesis Protocol for SNAP- and Halo-Tag-Based RNA Editing Tools.Molecules (Basel, Switzerland) · 2025Article
- Article
- Projection-Targeted Photopharmacology Reveals Distinct Anxiolytic Roles for Presynaptic mGluR2 in Prefrontal- and Insula-Amygdala Synapses.bioRxiv : the preprint server for biology · 2024Article
- A "double-edged" role for type-5 metabotropic glutamate receptors in pain disclosed by light-sensitive drugs.bioRxiv : the preprint server for biology · 2024Article
- Optical Approaches for Investigating Neuromodulation and G Protein-Coupled Receptor Signaling.Pharmacological reviews · 2023Review
- Optical Control of Dopamine D2-like Receptors with Cell-Specific Fast-Relaxing Photoswitches.Journal of the American Chemical Society · 2023Article
- Review
- Photoswitchable Serotonins for Optical Control of the 5-HTAngewandte Chemie (International ed. in English) · 2022Article
- Chemogenetics of cell surface receptors: beyond genetic and pharmacological approaches.RSC chemical biology · 2022Review
- The emergence of molecular systems neuroscience.Molecular brain · 2022Review
- Neurophotonic tools for microscopic measurements and manipulation: status report.Neurophotonics · 2022Article
- Modulating cell signalling in vivo with magnetic nanotransducers.Nature reviews. Methods primers · 2022Article
- Reagents and models for detecting endogenous GLP1R and GIPR.EBioMedicine · 2021Review
- A fine-tuned azobenzene for enhanced photopharmacology in vivo.Cell chemical biology · 2021Article
- Cell specific photoswitchable agonist for reversible control of endogenous dopamine receptors.Nature communications · 2021Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 3 countries.
Funding
Abstract
G protein-coupled receptor (GPCR) signaling occurs in complex spatiotemporal patterns that are difficult to probe using standard pharmacological and genetic approaches. A powerful approach for dissecting GPCRs is to use light-controlled pharmacological agents that are tethered covalently and specifically to genetically engineered receptors. However, deficits in our understanding of the mechanism of such photoswitches have limited application of this approach and its extension to other GPCRs. In this study, we have harnessed the power of bioorthogonal tethering to SNAP and CLIP protein tags to create a family of light-gated metabotropic glutamate receptors (mGluRs). We define the mechanistic determinants of photoswitch efficacy, including labeling efficiency, dependence on photoswitch structure, length dependence of the linker between the protein tag and the glutamate ligand, effective local concentration of the glutamate moiety, and affinity of the receptor for the ligand. We improve the scheme for photoswitch synthesis as well as photoswitch efficiency, and generate seven light-gated group II/III mGluRs, including variants of mGluR2, 3, 6, 7, and 8. Members of this family of light-controlled receptors can be used singly or in specifically labeled, independently light-controlled pairs for multiplexed control of receptor populations.
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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.