Plant-Derived Cyclotides Modulate κ-Opioid Receptor Signaling
Edin Muratspahić, Nataša Tomašević, S. Nasrollahi Shirazi, Jasmin Gattringer, Fabiola Susanna Emser, Michael Freissmuth, Christian W. Gruber
Abstract
or the potency and efficacy of U50,488 (a selective KOR agonist), respectively. In addition, T20K increased the basal response upon cotreatment with U50,488. In the bioluminescence resonance energy transfer assay T20K negatively modulated the efficacy of U50,488. This study identifies cyclotides capable of modulating KOR and highlights the potential of plant-derived peptides as an opportunity to develop cyclotide-based KOR modulators.
Topics & Concepts
G protein-coupled receptorAllosteric regulationAgonistPharmacologyReceptorBiochemistryBiologyChemistryBiochemical and Structural CharacterizationToxin Mechanisms and ImmunotoxinsPhytoplasmas and Hemiptera pathogens