ArticleBritish journal of pharmacology2016
Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Article in British journal of pharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 37 citations in OpenAlex.
- Molecular Crosstalk Between Intrauterine hCG and Endometrial Receptivity: Signalling Pathways, Immune Modulation, and Translational Perspectives in IVF.International journal of molecular sciences · 2025Review
- The Impact of Triptorelin on Hormone Levels in Human and Its Metabolite Confirmation Using Liquid Chromatography-Ion Trap/Time-of-Flight Mass Spectrometry (LC/MS-IT-TOF) and Liquid Chromatography-Orbitrap (LC-Orbitrap) for Doping Control Analysis.Drug testing and analysis · 2025Article
- A tool kit of highly selective and sensitive genetically encoded neuropeptide sensors.Science (New York, N.Y.) · 2023Article
- Perspective: Implications of Ligand-Receptor Binding Kinetics for Therapeutic Targeting of G Protein-Coupled Receptors.ACS pharmacology & translational science · 2020Review
- Fluorescent ligands: Bringing light to emerging GPCR paradigms.British journal of pharmacology · 2020Review
- Considerations for improved performance of competition association assays analysed with the Motulsky-Mahan's "kinetics of competitive binding" model.British journal of pharmacology · 2019Article
- A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine APurinergic signalling · 2019Article
- Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor.Scientific reports · 2019Article
- Binding kinetics of ligands acting at GPCRs.Molecular and cellular endocrinology · 2019Review
- In vitro and in silico analysis of the effects of DBritish journal of pharmacology · 2018Article
- A two-state model for the kinetics of competitive radioligand binding.British journal of pharmacology · 2018Article
- In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues.Journal of visualized experiments : JoVE · 2017Article
- Buserelin alleviates chloride transport defect in human cystic fibrosis nasal epithelial cells.PloS one · 2017Article
- Characterization of 12 GnRH peptide agonists - a kinetic perspective.British journal of pharmacology · 2016Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeDrug-target residence time is an important, yet often overlooked, parameter in drug discovery. Multiple studies have proposed an increased residence time to be beneficial for improved drug efficacy and/or longer duration of action. Currently, there are many drugs on the market targeting the gonadotropin-releasing hormone (GnRH) receptor for the treatment of hormone-dependent diseases. Surprisingly, the kinetic receptor-binding parameters of these analogues have not yet been reported. Therefore, this project focused on determining the receptor-binding kinetics of 12 GnRH peptide agonists, including many marketed drugs. EXPERIMENTAL APPROACH: A novel radioligand-binding competition association assay was developed and optimized for the human GnRH receptor with the use of a radiolabelled peptide agonist, [(125) I]-triptorelin. In addition to radioligand-binding studies, a homogeneous time-resolved FRET Tag-lite™ method was developed as an alternative assay for the same purpose. KEY
resultsTwo novel competition association assays were successfully developed and applied to determine the kinetic receptor-binding characteristics of 12 high-affinity GnRH peptide agonists. Results obtained from both methods were highly correlated. Interestingly, the binding kinetics of the peptide agonists were more divergent than their affinities with residence times ranging from 5.6 min (goserelin) to 125 min (deslorelin). CONCLUSIONS AND IMPLICATIONS: Our research provides new insights by incorporating kinetic, next to equilibrium, binding parameters in current research and development that can potentially improve future drug discovery targeting the GnRH receptor.
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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.