Publication | Open Access
Heterobivalent Ligands Crosslink Multiple Cell‐Surface Receptors: The Human Melanocortin‐4 and δ‐Opioid Receptors
68
Citations
13
References
2008
Year
Drug TargetSynthetic HeterobivalentPeptide SciencePharmacotherapyMolecular PharmacologyHormone Analogue MshCell SignalingBiochemistryG Protein-coupled ReceptorReceptor (Biochemistry)Mechanism Of ActionNeuropharmacologyNon-peptide LigandPharmacologyδ-Opioid Ligand Deltorphin-iiCell BiologyHuman Melanocortin‐4Signal Transductionδ‐Opioid ReceptorsFunctional SelectivityNatural SciencesNeuropeptide ReceptorMedicineSmall MoleculesDrug DiscoveryQuantitative Pharmacology
Together we bind: A series of synthetic heterobivalent ligands containing a fragment of melanocyte stimulating hormone analogue MSH(7) and the δ-opioid ligand deltorphin-II has been prepared. These ligands bind with higher affinity and with apparent cooperativity to cells expressing both hMC4R and δ-opioid receptors. Binding affinities were evaluated using a lanthanide-based in-cyto time-resolved fluorescence binding assay. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2008/z702770_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
| Year | Citations | |
|---|---|---|
Page 1
Page 1