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Endomorphin-2: a biased agonist at the mu-opioid receptor.
Rivero G, Llorente J, McPherson J, Cooke A, Mundell SJ, McArdle CA, Rosethorne EM, Charlton SJ, Krasel C, Bailey CP, Henderson G, Kelly E. Rivero G, et al. Mol Pharmacol. 2012 Aug;82(2):178-88. doi: 10.1124/mol.112.078659. Epub 2012 May 2. Mol Pharmacol. 2012. PMID: 22553358 Free PMC article.
Previously we correlated the efficacy for G protein activation with that for arrestin recruitment for a number of agonists at the mu-opioid receptor (MOPr) stably expressed in HEK293 cells. We suggested that the endomorphins (endomorphin-1 and -2) migh …
Previously we correlated the efficacy for G protein activation with that for arrestin recruitment for a number of agonists at the …
Functional selectivity of EM-2 analogs at the mu-opioid receptor.
Piekielna-Ciesielska J, Malfacini D, Djeujo FM, Marconato C, Wtorek K, Calo' G, Janecka A. Piekielna-Ciesielska J, et al. Front Pharmacol. 2023 Feb 24;14:1133961. doi: 10.3389/fphar.2023.1133961. eCollection 2023. Front Pharmacol. 2023. PMID: 36909169 Free PMC article.
The mu opioid receptor agonists are the most efficacious pain controlling agents but their use is accompanied by severe side effects. ...The data presented here contribute to our understanding of EM-2 interaction with the mu opioid rec …
The mu opioid receptor agonists are the most efficacious pain controlling agents but their use is accompanied by …
The endomorphin-1/2 and dynorphin-B peptides display biased agonism at the mu opioid receptor.
LaVigne J, Keresztes A, Chiem D, Streicher JM. LaVigne J, et al. Pharmacol Rep. 2020 Apr;72(2):465-471. doi: 10.1007/s43440-020-00061-x. Epub 2020 Feb 28. Pharmacol Rep. 2020. PMID: 32112361
BACKGROUND: Opioid agonist activation at the mu opioid receptor (MOR) can lead to a wide variety of physiological responses. Many opioid agonists share the ability to selectively and preferentially activate specific signaling pathw …
BACKGROUND: Opioid agonist activation at the mu opioid receptor (MOR) can lead to a wide variety of physi …
A tetrapeptide class of biased analgesics from an Australian fungus targets the -opioid receptor.
Dekan Z, Sianati S, Yousuf A, Sutcliffe KJ, Gillis A, Mallet C, Singh P, Jin AH, Wang AM, Mohammadi SA, Stewart M, Ratnayake R, Fontaine F, Lacey E, Piggott AM, Du YP, Canals M, Sessions RB, Kelly E, Capon RJ, Alewood PF, Christie MJ. Dekan Z, et al. Proc Natl Acad Sci U S A. 2019 Oct 29;116(44):22353-22358. doi: 10.1073/pnas.1908662116. Epub 2019 Oct 14. Proc Natl Acad Sci U S A. 2019. PMID: 31611414 Free PMC article.
Given their resemblance to known short peptide opioid agonists, we elucidated that they were weak (K(i) low micromolar) mu-opioid agonists, which led to the design of bilorphin, a potent and selective mu-opioid receptor (MOP …
Given their resemblance to known short peptide opioid agonists, we elucidated that they were weak (K(i) low micromolar) mu …
Intracerebroventricular administration of CYX-6, a potent mu-opioid receptor agonist, a delta- and kappa-opioid receptor antagonist and a biased ligand at mu, delta & kappa-opioid receptors, evokes antinociception with minimal constipation and respiratory depression in rats in contrast to morphine.
Imam MZ, Kuo A, Ghassabian S, Cai Y, Qin Y, Li T, Smith MT. Imam MZ, et al. Eur J Pharmacol. 2020 Mar 15;871:172918. doi: 10.1016/j.ejphar.2020.172918. Epub 2020 Jan 17. Eur J Pharmacol. 2020. PMID: 31958457
Mu opioid receptor (MOPr) agonists are thought to produce analgesia via modulation of G-protein-coupled intracellular signalling pathways whereas the beta-arrestin2 pathway is proposed to mediate opioid-related adverse effects. Here, we report t …
Mu opioid receptor (MOPr) agonists are thought to produce analgesia via modulation of G-protein-coupled intracel …
Plasticity of Signaling by Spinal Estrogen Receptor alpha, kappa-Opioid Receptor, and Metabotropic Glutamate Receptors over the Rat Reproductive Cycle Regulates Spinal Endomorphin 2 Antinociception: Relevance of Endogenous-Biased Agonism.
Liu NJ, Murugaiyan V, Storman EM, Schnell SA, Kumar A, Wessendorf MW, Gintzler AR. Liu NJ, et al. J Neurosci. 2017 Nov 15;37(46):11181-11191. doi: 10.1523/JNEUROSCI.1927-17.2017. Epub 2017 Oct 12. J Neurosci. 2017. PMID: 29025923 Free PMC article.
We previously showed that intrathecal application of endomorphin 2 [EM2; the highly specific endogenous mu-opioid receptor (MOR) ligand] induces antinociception that varies with stage of the rat estrous cycle: minimal during diestrus and promine …
We previously showed that intrathecal application of endomorphin 2 [EM2; the highly specific endogenous mu-opioid …
Sequence-Specific Regulation of Endocytic Lifetimes Modulates Arrestin-Mediated Signaling at the Opioid Receptor.
Weinberg ZY, Zajac AS, Phan T, Shiwarski DJ, Puthenveedu MA. Weinberg ZY, et al. Mol Pharmacol. 2017 Apr;91(4):416-427. doi: 10.1124/mol.116.106633. Epub 2017 Feb 2. Mol Pharmacol. 2017. PMID: 28153854 Free PMC article.
Functional selectivity at the opioid receptor ( R), a prototypical G-protein-coupled receptor that is a physiologically relevant target for endogenous opioid neurotransmitters and analgesics, has been a major focus for drug discovery in the recent pa …
Functional selectivity at the opioid receptor ( R), a prototypical G-protein-coupled receptor that is a physiological …
Biased mu-opioid receptor agonists diversely regulate lateral mobility and functional coupling of the receptor to its cognate G proteins.
Melkes B, Hejnova L, Novotny J. Melkes B, et al. Naunyn Schmiedebergs Arch Pharmacol. 2016 Dec;389(12):1289-1300. doi: 10.1007/s00210-016-1293-8. Epub 2016 Sep 6. Naunyn Schmiedebergs Arch Pharmacol. 2016. PMID: 27600870
There are some indications that biased mu-opioid ligands may diversely affect mu-opioid receptor (MOR) properties. Here, we used confocal fluorescence recovery after photobleaching (FRAP) to study the regulation by different MOR agonis …
There are some indications that biased mu-opioid ligands may diversely affect mu-opioid receptor ( …
Residues W320 and Y328 within the binding site of the mu-opioid receptor influence opiate ligand bias.
Hothersall JD, Torella R, Humphreys S, Hooley M, Brown A, McMurray G, Nickolls SA. Hothersall JD, et al. Neuropharmacology. 2017 May 15;118:46-58. doi: 10.1016/j.neuropharm.2017.03.007. Epub 2017 Mar 7. Neuropharmacology. 2017. PMID: 28283391 Free article.
The development of G protein-biased agonists for the mu-opioid receptor (MOR) offers a clear drug discovery rationale for improved analgesia and reduced side-effects of opiate pharmacotherapy. ...In contrast, endomorphin-1 gained activity with Y …
The development of G protein-biased agonists for the mu-opioid receptor (MOR) offers a clear drug discove …
Ligand-specific regulation of the endogenous mu-opioid receptor by chronic treatment with mu-opioid peptide agonists.
Murányi M, Cinar R, Kékesi O, Birkás E, Fábián G, Bozó B, Zentai A, Tóth G, Kicsi EG, Mácsai M, Dochnal R, Szabó G, Szücs M. Murányi M, et al. Biomed Res Int. 2013;2013:501086. doi: 10.1155/2013/501086. Epub 2013 Nov 24. Biomed Res Int. 2013. PMID: 24350273 Free PMC article.
Since the discovery of the endomorphins (EM), the postulated endogenous peptide agonists of the mu-opioid receptors, several analogues have been synthesized to improve their binding and pharmacological profiles. We have shown previously that a new anal …
Since the discovery of the endomorphins (EM), the postulated endogenous peptide agonists of the mu-opioid receptors …
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