ArticleScientific reports2015
Endogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 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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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
21 citing papers in PubMed, 51 citations in OpenAlex.
- Deep learning reveals endogenous sterols as allosteric modulators of the GPCR-Gα interface.eLife · 2025Article
- The NPXXY Motif Regulates β-Arrestin Recruitment by the CB1 Cannabinoid Receptor.Cannabis and cannabinoid research · 2023Article
- Application of Mixed-Solvent Molecular Dynamics Simulations for Prediction of Allosteric Sites on G Protein-Coupled Receptors.Molecular pharmacology · 2023Article
- Evaluating Allosteric Perturbations in Cannabinoid Receptor 1 byACS omega · 2022Article
- Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of Cannabinoid CB1 Receptor Bound to a Negative Allosteric Modulator, ORG27569, and Analogs.Journal of medicinal chemistry · 2022Article
- Covalent cannabinoid receptor ligands - structural insight and selectivity challenges.RSC medicinal chemistry · 2022Review
- G-Protein-Coupled Receptors and Ischemic Stroke: a Focus on Molecular Function and Therapeutic Potential.Molecular neurobiology · 2021Review
- Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.Bioorganic & medicinal chemistry · 2021Article
- G protein-coupled receptors: structure- and function-based drug discovery.Signal transduction and targeted therapy · 2021Review
- Covalent allosteric modulation: An emerging strategy for GPCRs drug discovery.European journal of medicinal chemistry · 2020Review
- Structure of an allosteric modulator bound to the CB1 cannabinoid receptor.Nature chemical biology · 2019Article
- The Endocannabinoid System as a Target in Cancer Diseases: Are We There Yet?Frontiers in pharmacology · 2019Review
- Potential for endocannabinoid system modulation in ocular pain and inflammation: filling the gaps in current pharmacological options.Neuronal signaling · 2018Review
- Allosteric modulators of cannabinoid receptor 1: developing compounds for improved specificity.Drug metabolism reviews · 2018Review
- Disordered Peptides Looking for Their Native Environment: Structural Basis of CB1 Endocannabinoid Receptor Binding to Pepcans.Frontiers in molecular biosciences · 2018Article
- Modulation of CB1 cannabinoid receptor by allosteric ligands: Pharmacology and therapeutic opportunities.Neuropharmacology · 2017Review
- Allosteric Modulation: An Alternate Approach Targeting the Cannabinoid CB1 Receptor.Medicinal research reviews · 2017Review
- Assessing Allosteric Modulation of CBMethods in enzymology · 2017Article
- Leveraging allostery to improve G protein-coupled receptor (GPCR)-directed therapeutics: cannabinoid receptor 1 as discovery target.Expert opinion on drug discovery · 2016Review
- Effect of N-arachidonoyl-l-serine on human cerebromicrovascular endothelium.Biochemistry and biophysics reports · 2016Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A Cannabinoid Receptor 1 (CB1) binding site for the selective allosteric modulator ORG27569 is here identified through an integrate approach of consensus pocket prediction, mutagenesis studies and Mass Spectrometry. This unprecedented ORG27569 pocket presents the structural features of a Cholesterol Consensus Motif, a cholesterol interacting region already found in other GPCRs. ORG27569 and cholesterol affects oppositely CB1 affinity for orthosteric ligands. Moreover, the rise in cholesterol intracellular level results in CB1 trafficking to the axonal region of neuronal cells, while, on the contrary, ORG27568 binding induces CB1 enrichment at the soma. This control of receptor migration among functionally different membrane regions of the cell further contributes to downstream signalling and adds a previously unknown mechanism underpinning CB1 modulation by ORG27569 , that goes beyond a mere control of receptor affinity for orthosteric ligands.
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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.