ArticleStructure (London, England : 1993)2015
The Importance of Ligand-Receptor Conformational Pairs in Stabilization: Spotlight on the N/OFQ G Protein-Coupled Receptor.
Article in Structure (London, England : 1993), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers, 1 of them a synthesis that pooled it.
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Who cites it
35 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Nociceptin/orphanin FQ receptor ligands and translational challenges: focus on cebranopadol as an innovative analgesic.British journal of anaesthesia · 2018Pooled it
- Identification of small molecule ligands for GPR83 that modulate morphine antinociception and reward.Molecular pharmacology · 2026Article
- Synthesis and Pharmacological Characterization of Nociceptin/Orphanin FQ Dimeric Ligands.Journal of medicinal chemistry · 2025Article
- G Protein-Coupled Receptor-Ligand Pose and Functional Class Prediction.International journal of molecular sciences · 2024Article
- Involvement of the Opioid Peptide Family in Cancer Progression.Biomedicines · 2023Review
- Synthesis, Biological Activity and Molecular Docking of Chimeric Peptides Targeting Opioid and NOP Receptors.International journal of molecular sciences · 2022Article
- Structure Prediction, Evaluation, and Validation of GPR18 Lipid Receptor Using Free Programs.International journal of molecular sciences · 2022Article
- Universal platform for the generation of thermostabilized GPCRs that crystallize in LCP.Nature protocols · 2022Review
- Mechanistic Characterization of the Pharmacological Profile of HS-731, a Peripherally Acting Opioid Analgesic, at the µ-, δ-, κ-Opioid and Nociceptin Receptors.Molecules (Basel, Switzerland) · 2022Article
- Spotlight on Nociceptin/Orphanin FQ Receptor in the Treatment of Pain.Molecules (Basel, Switzerland) · 2022Review
- Novel Molecular Targets of Antidepressants.Molecules (Basel, Switzerland) · 2022Review
- Article
- The Buprenorphine Analogue BU10119 Attenuates Drug-Primed and Stress-Induced Cocaine Reinstatement in Mice.The Journal of pharmacology and experimental therapeutics · 2021Article
- Antinociceptive Efficacy of the µ-Opioid/Nociceptin Peptide-Based Hybrid KGNOP1 in Inflammatory Pain without Rewarding Effects in Mice: An Experimental Assessment and Molecular Docking.Molecules (Basel, Switzerland) · 2021Article
- Structure-Based SAR in the Design of Selective or Bifunctional Nociceptin (NOP) Receptor Agonists.The AAPS journal · 2021Article
- Hair graying with aging in mice carrying oncogenic RET.Aging cell · 2020Article
- Biased Agonism at Nociceptin/Orphanin FQ Receptors: A Structure Activity Study on N/OFQ(1-13)-NHJournal of medicinal chemistry · 2020Article
- Structural biology of human GPCR drugs and endogenous ligands - insights from NMR spectroscopy.Methods (San Diego, Calif.) · 2020Review
- Nociceptin/Orphanin FQ Peptide Receptor-Related Ligands as Novel Analgesics.Current topics in medicinal chemistry · 2020Review
- Genetic basis of functional variability in adhesion G protein-coupled receptors.Scientific reports · 2019Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
Understanding the mechanism by which ligands affect receptor conformational equilibria is key in accelerating membrane protein structural biology. In the case of G protein-coupled receptors (GPCRs), we currently pursue a brute-force approach for identifying ligands that stabilize receptors and facilitate crystallogenesis. The nociceptin/orphanin FQ peptide receptor (NOP) is a member of the opioid receptor subfamily of GPCRs for which many structurally diverse ligands are available for screening. We observed that antagonist potency is correlated with a ligand's ability to induce receptor stability (Tm) and crystallogenesis. Using this screening strategy, we solved two structures of NOP in complex with top candidate ligands SB-612111 and C-35. Docking studies indicate that while potent, stabilizing antagonists strongly favor a single binding orientation, less potent ligands can adopt multiple binding modes, contributing to their low Tm values. These results suggest a mechanism for ligand-aided crystallogenesis whereby potent antagonists stabilize a single ligand-receptor conformational pair.
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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.