ArticleScience signaling2017
Subtle modifications to oxytocin produce ligands that retain potency and improved selectivity across species.
Article in Science signaling, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 76 citations in OpenAlex.
- Fluorescent Peptide Tracers for Simultaneous Oxytocin Receptor Activation and Visualization.Angewandte Chemie (International ed. in English) · 2025Article
- Development and characterisation of novel oxytocin analogues for PET imaging.Communications chemistry · 2025Article
- An Efficient Thiol-ene Mediated Protocol for Thiolated Peptide Synthesis and On-Resin Diversification.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Site-selectiveChemical science · 2024Article
- Late-stageChemical science · 2024Article
- Targeting the Oxytocin Receptor for Breast Cancer Management: A Niche for Peptide Tracers.Journal of medicinal chemistry · 2024Review
- Photoswitchable Probes of Oxytocin and Vasopressin.Journal of medicinal chemistry · 2023Article
- An analgesic pathway from parvocellular oxytocin neurons to the periaqueductal gray in rats.Nature communications · 2023Article
- Structure-Based Design of Glycosylated Oxytocin Analogues with Improved Selectivity and Antinociceptive Activity.ACS medicinal chemistry letters · 2023Article
- High Oxytocin Receptor Expression Linked to Increased Cell Migration and Reduced Survival in Patients with Triple-Negative Breast Cancer.Biomedicines · 2022Article
- Improving the Gastrointestinal Stability of Linaclotide.Journal of medicinal chemistry · 2021Article
- Nature-inspired dimerization as a strategy to modulate neuropeptide pharmacology exemplified with vasopressin and oxytocin.Chemical science · 2021Article
- Neuropeptide signalling systems - An underexplored target for venom drug discovery.Biochemical pharmacology · 2020Review
- Review
- Oxytocin in the Male Reproductive Tract; The Therapeutic Potential of Oxytocin-Agonists and-Antagonists.Frontiers in endocrinology · 2020Review
- I8-arachnotocin-an arthropod-derived G protein-biased ligand of the human vasopressin VScientific reports · 2019Article
- LeuScientific reports · 2019Article
- Nature-Derived Peptides: A Growing Niche for GPCR Ligand Discovery.Trends in pharmacological sciences · 2019Review
- Oxytocin structure and function in New World monkeys: from pharmacology to behavior.Integrative zoology · 2018Review
- Binding Characteristics of Two Oxytocin Variants and Vasopressin at Oxytocin Receptors from Four Primate Species with Different Social Behavior Patterns.The Journal of pharmacology and experimental therapeutics · 2018Article
Corrections and comments
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Authors and funding
18 authors at 7 institutions in 6 countries.
Funding
Abstract
Oxytocin and vasopressin mediate various physiological functions that are important for osmoregulation, reproduction, cardiovascular function, social behavior, memory, and learning through four G protein-coupled receptors that are also implicated in high-profile disorders. Targeting these receptors is challenging because of the difficulty in obtaining ligands that retain selectivity across rodents and humans for translational studies. We identified a selective and more stable oxytocin receptor (OTR) agonist by subtly modifying the pharmacophore framework of human oxytocin and vasopressin. [Se-Se]-oxytocin-OH displayed similar potency to oxytocin but improved selectivity for OTR, an effect that was retained in mice. Centrally infused [Se-Se]-oxytocin-OH potently reversed social fear in mice, confirming that this action was mediated by OTR and not by V1a or V1b vasopressin receptors. In addition, [Se-Se]-oxytocin-OH produced a more regular contraction pattern than did oxytocin in a preclinical labor induction and augmentation model using myometrial strips from cesarean sections. [Se-Se]-oxytocin-OH had no activity in human cardiomyocytes, indicating a potentially improved safety profile and therapeutic window compared to those of clinically used oxytocin. In conclusion, [Se-Se]-oxytocin-OH is a novel probe for validating OTR as a therapeutic target in various biological systems and is a promising new lead for therapeutic development. Our medicinal chemistry approach may also be applicable to other peptidergic signaling systems with similar selectivity issues.
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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.