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1,242 results

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Page 1
Biased Opioid Ligands.
Faouzi A, Varga BR, Majumdar S. Faouzi A, et al. Molecules. 2020 Sep 16;25(18):4257. doi: 10.3390/molecules25184257. Molecules. 2020. PMID: 32948048 Free PMC article. Review.
Four types of opioid receptors have been described, including the mu-opioid receptor (MOR), kappa-opioid receptor (KOR), delta-opioid receptor (DOR), and the nociceptin opioid peptide receptor (NOP receptor). ...It has been proposed that ligands not recruiting beta-arresti …
Four types of opioid receptors have been described, including the mu-opioid receptor (MOR), kappa-opioid receptor (KOR), delta-opioid …
Peptide-Liganded G Protein-Coupled Receptors as Neurotherapeutics.
Eiden LE, Goosens KA, Jacobson KA, Leggio L, Zhang L. Eiden LE, et al. ACS Pharmacol Transl Sci. 2020 Mar 18;3(2):190-202. doi: 10.1021/acsptsci.0c00017. eCollection 2020 Apr 10. ACS Pharmacol Transl Sci. 2020. PMID: 32296762 Free PMC article. Review.
Peptide-liganded G protein-coupled receptors (GPCRs) are a growing fraction of GPCR drug targets, concentrated in two of the five major GPCR structural classes. The basic physiology and pharmacology of some within the rhodopsin class, for example, the enkephalin (mu opioid …
Peptide-liganded G protein-coupled receptors (GPCRs) are a growing fraction of GPCR drug targets, concentrated in two of the five maj …
betagamma G-proteins, but not regulators of G-protein signaling 4, modulate opioid-induced respiratory rate depression.
Danaf J, da Silveira Scarpellini C, Montandon G. Danaf J, et al. Front Physiol. 2023 Apr 6;14:1043581. doi: 10.3389/fphys.2023.1043581. eCollection 2023. Front Physiol. 2023. PMID: 37089428 Free PMC article.
Most opioid drugs, such as fentanyl, act on opioid receptors such as the G-protein-coupled -opioid receptors (MOR). G-protein-coupled receptors activate pertussis toxin-sensitive G-proteins to inhibit neuronal activity. Binding of opioid ligands to …
Most opioid drugs, such as fentanyl, act on opioid receptors such as the G-protein-coupled -opioid receptors (MOR). G-p …
Pharmacological and Physicochemical Properties Optimization for Dual-Target Dopamine D(3) (D(3)R) and mu-Opioid (MOR) Receptor Ligands as Potentially Safer Analgesics.
Bonifazi A, Saab E, Sanchez J, Nazarova AL, Zaidi SA, Jahan K, Katritch V, Canals M, Lane JR, Newman AH. Bonifazi A, et al. J Med Chem. 2023 Aug 10;66(15):10304-10341. doi: 10.1021/acs.jmedchem.3c00417. Epub 2023 Jul 19. J Med Chem. 2023. PMID: 37467430
A new generation of dual-target mu opioid receptor (MOR) agonist/dopamine D(3) receptor (D(3)R) antagonist/partial agonists with optimized physicochemical properties was designed and synthesized. Combining in vitro cell-based on-target/off-target affinity screening, in sil …
A new generation of dual-target mu opioid receptor (MOR) agonist/dopamine D(3) receptor (D(3)R) antagonist/partial agonists with opti …
Ligand-Free Signaling of G-Protein-Coupled Receptors: Relevance to mu Opioid Receptors in Analgesia and Addiction.
Sadee W, McKew JC. Sadee W, et al. Molecules. 2022 Sep 8;27(18):5826. doi: 10.3390/molecules27185826. Molecules. 2022. PMID: 36144565 Free PMC article. Review.
In addition, agonists bind to MOR but can dissociate upon MOR activation, with ligand-free MOR-mu* carrying out signaling. ...Antagonists competitively prevent resting MOR (MOR-mu) activation to MOR-mu*, while common antagonists, such as …
In addition, agonists bind to MOR but can dissociate upon MOR activation, with ligand-free MOR-mu* carrying out signali …
Synthesis, biological, and structural explorations of a series of mu-opioid receptor (MOR) agonists with high G protein signaling bias.
Yang Y, Wang Y, Zuo A, Li C, Wang W, Jiang W, Zhang X, Che X, Zhang Y, Wu W, Cen X, Wang H, Tian J. Yang Y, et al. Eur J Med Chem. 2022 Jan 15;228:113986. doi: 10.1016/j.ejmech.2021.113986. Epub 2021 Nov 12. Eur J Med Chem. 2022. PMID: 34802839
Biased agonism refers to the ability of compounds to drive preferred signaling pathways and avoid adverse signaling pathways in a ligand-dependent manner for some G-protein-coupled receptors. It is thought that the separation of therapeutic efficacy (e.g., analgesia …
Biased agonism refers to the ability of compounds to drive preferred signaling pathways and avoid adverse signaling pathways in a ligand-dep …
Regulator of G-Protein Signaling (RGS) Protein Modulation of Opioid Receptor Signaling as a Potential Target for Pain Management.
Senese NB, Kandasamy R, Kochan KE, Traynor JR. Senese NB, et al. Front Mol Neurosci. 2020 Jan 24;13:5. doi: 10.3389/fnmol.2020.00005. eCollection 2020. Front Mol Neurosci. 2020. PMID: 32038168 Free PMC article. Review.
All clinically available opioid analgesics bind to and activate the mu-opioid receptor (MOR), a heterotrimeric G-protein-coupled receptor, to produce analgesia. ...These proteins act as negative regulators of G-protein signaling by serving as GTPase accelerat …
All clinically available opioid analgesics bind to and activate the mu-opioid receptor (MOR), a heterotrimeric G-protein-coupl …
Mu-opioid receptor selective superagonists produce prolonged respiratory depression.
Malcolm NJ, Palkovic B, Sprague DJ, Calkins MM, Lanham JK, Halberstadt AL, Stucke AG, McCorvy JD. Malcolm NJ, et al. iScience. 2023 Jun 13;26(7):107121. doi: 10.1016/j.isci.2023.107121. eCollection 2023 Jul 21. iScience. 2023. PMID: 37416459 Free PMC article.
Synthetic opioids are increasingly challenging to combat the opioid epidemic and act primarily at opioid receptors, chiefly the G protein-coupled receptor (GPCR) mu-opioid receptor (MOR), which signals through G protein-dependent and beta-arrestin pathways. . …
Synthetic opioids are increasingly challenging to combat the opioid epidemic and act primarily at opioid receptors, chiefly the G pro …
Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias.
Kennedy NM, Schmid CL, Ross NC, Lovell KM, Yue Z, Chen YT, Cameron MD, Bohn LM, Bannister TD. Kennedy NM, et al. J Med Chem. 2018 Oct 11;61(19):8895-8907. doi: 10.1021/acs.jmedchem.8b01136. Epub 2018 Sep 24. J Med Chem. 2018. PMID: 30199635 Free PMC article.
Substantial data now exists to support the premise that G protein signaling biased MOR agonists can be effective analgesic agents. ...Herein we describe the synthesis and optimization of piperidine benzimidazolone MOR agonists that together display a wide ran …
Substantial data now exists to support the premise that G protein signaling biased MOR agonists can be effective analgesic age …
Current strategies toward safer mu opioid receptor drugs for pain management.
Ehrlich AT, Kieffer BL, Darcq E. Ehrlich AT, et al. Expert Opin Ther Targets. 2019 Apr;23(4):315-326. doi: 10.1080/14728222.2019.1586882. Epub 2019 Mar 15. Expert Opin Ther Targets. 2019. PMID: 30802415 Free PMC article. Review.
Areas covered: Ongoing efforts to generate safer opioid analgesics are reviewed here. The design of biased compounds that trigger MOR induced G protein over beta-arrestin signaling, peripheral opioids, drugs targeting MORs in heteromers and drugs enhancing endogenou …
Areas covered: Ongoing efforts to generate safer opioid analgesics are reviewed here. The design of biased compounds that trigger MOR …
1,242 results