Nociceptin/Orphanin FQ Receptor Antibodies
The nociceptin/orphanin FQ receptor (NFQ receptor, NOP) is the fourth discovered member of the opioid receptor family. Bifunctional agonists that target NOP and MOP such as cebranopadol or AT-121 are under active investigation as novel analgesics with fewer side effects. NOP desensitization, trafficking and signaling are regulated by phosphorylation of carboxyl-terminal serine346 (pS346-NOP), serine351 (pS351-NOP) and threonine362/serine363 (pT362/pS363-NOP) residues. Agonist-induced NOP phosphorylation is predominantly mediated by GRK2 and GRK3. S346 and S351 are also substrates for PKC-mediated phosphorylation. The nomenclature refers to the human NOP. This phosphorylation motif is also present in mice and rats. For more information on NFQ receptor pharmacology please refer to the IUPHAR database. For further reading refer to:
Mann A, Moulédous L, Froment C, O'Neill PR, Dasgupta P, Günther T, Brunori G, Kieffer BL, Toll L, Bruchas MR, Zaveri NT, Schulz S. Agonist-selective NOP receptor phosphorylation correlates in vitro and in vivo and reveals differential post-activation signaling by chemically diverse agonists. Sci Signal. 2019 Mar 26;12(574). pii: eaau8072. doi: 10.1126/scisignal.aau8072. PubMed PMID: 30914485; PubMed Central PMCID: PMC6934085.
Toll L, Bruchas MR, Calo' G, Cox BM, Zaveri NT. Nociceptin/Orphanin FQ Receptor Structure, Signaling, Ligands, Functions, and Interactions with Opioid Systems. Pharmacol Rev. 2016 Apr;68(2):419-57. doi: 10.1124/pr.114.009209. Epub 2016 Mar 8. Review. PubMed PMID: 26956246; PubMed Central PMCID: PMC4813427.