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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.

Front Mol Neurosci. 2020 Jan 24;13:5. doi: 10.3389/fnmol.2020.00005. eCollection 2020. Review.


Aromatic-Amine Pendants Produce Highly Potent and Efficacious Mixed Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Peptidomimetics with Enhanced Metabolic Stability.

Henry S, Anand JP, Twarozynski JJ, Brinkel AC, Pogozheva ID, Sears BF, Jutkiewicz EM, Traynor JR, Mosberg HI.

J Med Chem. 2020 Feb 27;63(4):1671-1683. doi: 10.1021/acs.jmedchem.9b01818. Epub 2020 Feb 10.


Structure-Activity Relationships of 7-Substituted Dimethyltyrosine-Tetrahydroisoquinoline Opioid Peptidomimetics.

Montgomery D, Anand JP, Baber MA, Twarozynski JJ, Hartman JG, Delong LJ, Traynor JR, Mosberg HI.

Molecules. 2019 Nov 26;24(23). pii: E4302. doi: 10.3390/molecules24234302.


Novel Dimethyltyrosine-Tetrahydroisoquinoline Peptidomimetics with Aromatic Tetrahydroisoquinoline Substitutions Show in Vitro Kappa and Mu Opioid Receptor Agonism.

Montgomery D, Anand JP, Griggs NW, Fernandez TJ, Hartman JG, Sánchez-Santiago AA, Pogozheva ID, Traynor JR, Mosberg HI.

ACS Chem Neurosci. 2019 Aug 21;10(8):3682-3689. doi: 10.1021/acschemneuro.9b00250. Epub 2019 Jul 1.


Structural Simplification of a Tetrahydroquinoline-Core Peptidomimetic μ-Opioid Receptor (MOR) Agonist/δ-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability.

Henry SP, Fernandez TJ, Anand JP, Griggs NW, Traynor JR, Mosberg HI.

J Med Chem. 2019 Apr 25;62(8):4142-4157. doi: 10.1021/acs.jmedchem.9b00219. Epub 2019 Apr 12.


Dual Pharmacophores Explored via Structure-Activity Relationship (SAR) Matrix: Insights into Potent, Bifunctional Opioid Ligand Design.

Nastase AF, Anand JP, Bender AM, Montgomery D, Griggs NW, Fernandez TJ, Jutkiewicz EM, Traynor JR, Mosberg HI.

J Med Chem. 2019 Apr 25;62(8):4193-4203. doi: 10.1021/acs.jmedchem.9b00378. Epub 2019 Apr 9.


The δ-opioid receptor positive allosteric modulator BMS 986187 is a G-protein-biased allosteric agonist.

Stanczyk MA, Livingston KE, Chang L, Weinberg ZY, Puthenveedu MA, Traynor JR.

Br J Pharmacol. 2019 Jun;176(11):1649-1663. doi: 10.1111/bph.14602. Epub 2019 Apr 14.


The Role of G-proteins and G-protein Regulating Proteins in Depressive Disorders.

Senese NB, Rasenick MM, Traynor JR.

Front Pharmacol. 2018 Nov 13;9:1289. doi: 10.3389/fphar.2018.01289. eCollection 2018. Review.


Role of hippocampal 5-HT1A receptors in the antidepressant-like phenotype of mice expressing RGS-insensitive Gαi2 protein.

Senese NB, Oginsky M, Neubig RR, Ferrario C, Jutkiewicz EM, Traynor JR.

Neuropharmacology. 2018 Oct;141:296-304. doi: 10.1016/j.neuropharm.2018.09.002. Epub 2018 Sep 4.


Regulators of G-Protein Signaling (RGS) Proteins Promote Receptor Coupling to G-Protein-Coupled Inwardly Rectifying Potassium (GIRK) Channels.

McPherson KB, Leff ER, Li MH, Meurice C, Tai S, Traynor JR, Ingram SL.

J Neurosci. 2018 Oct 10;38(41):8737-8744. doi: 10.1523/JNEUROSCI.0516-18.2018. Epub 2018 Aug 27.


Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor.

Livingston KE, Mahoney JP, Manglik A, Sunahara RK, Traynor JR.

Elife. 2018 Jun 22;7. pii: e32499. doi: 10.7554/eLife.32499.


Synthesis and Pharmacological Evaluation of Novel C-8 Substituted Tetrahydroquinolines as Balanced-Affinity Mu/Delta Opioid Ligands for the Treatment of Pain.

Nastase AF, Griggs NW, Anand JP, Fernandez TJ, Harland AA, Trask TJ, Jutkiewicz EM, Traynor JR, Mosberg HI.

ACS Chem Neurosci. 2018 Jul 18;9(7):1840-1848. doi: 10.1021/acschemneuro.8b00139. Epub 2018 May 2.


In vivo effects of μ-opioid receptor agonist/δ-opioid receptor antagonist peptidomimetics following acute and repeated administration.

Anand JP, Kochan KE, Nastase AF, Montgomery D, Griggs NW, Traynor JR, Mosberg HI, Jutkiewicz EM.

Br J Pharmacol. 2018 Jun;175(11):2013-2027. doi: 10.1111/bph.14148. Epub 2018 Apr 24.


Role of signalling molecules in behaviours mediated by the δ opioid receptor agonist SNC80.

Dripps IJ, Boyer BT, Neubig RR, Rice KC, Traynor JR, Jutkiewicz EM.

Br J Pharmacol. 2018 Mar;175(6):891-901. doi: 10.1111/bph.14131. Epub 2018 Feb 9.


Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors.

Livingston KE, Stanczyk MA, Burford NT, Alt A, Canals M, Traynor JR.

Mol Pharmacol. 2018 Feb;93(2):157-167. doi: 10.1124/mol.117.109561. Epub 2017 Dec 12.


Role of the guanine nucleotide binding protein, Gαo, in the development of morphine tolerance and dependence.

Lamberts JT, Rosenthal LD, Jutkiewicz EM, Traynor JR.

Psychopharmacology (Berl). 2018 Jan;235(1):71-82. doi: 10.1007/s00213-017-4742-2. Epub 2017 Oct 3.


Placement of Hydroxy Moiety on Pendant of Peptidomimetic Scaffold Modulates Mu and Kappa Opioid Receptor Efficacy.

Harland AA, Pogozheva ID, Griggs NW, Trask TJ, Traynor JR, Mosberg HI.

ACS Chem Neurosci. 2017 Nov 15;8(11):2549-2557. doi: 10.1021/acschemneuro.7b00284. Epub 2017 Aug 25.


Allostery at opioid receptors: modulation with small molecule ligands.

Livingston KE, Traynor JR.

Br J Pharmacol. 2018 Jul;175(14):2846-2856. doi: 10.1111/bph.13823. Epub 2017 Jun 7. Review.


Modulation of opioid receptor affinity and efficacy via N-substitution of 9β-hydroxy-5-(3-hydroxyphenyl)morphan: Synthesis and computer simulation study.

Truong PM, Hassan SA, Lee YS, Kopajtic TA, Katz JL, Chadderdon AM, Traynor JR, Deschamps JR, Jacobson AE, Rice KC.

Bioorg Med Chem. 2017 Apr 15;25(8):2406-2422. doi: 10.1016/j.bmc.2017.02.064. Epub 2017 Mar 1.


Benzylideneoxymorphone: A new lead for development of bifunctional mu/delta opioid receptor ligands.

Healy JR, Bezawada P, Griggs NW, Devereaux AL, Matsumoto RR, Traynor JR, Coop A, Cunningham CW.

Bioorg Med Chem Lett. 2017 Feb 1;27(3):666-669. doi: 10.1016/j.bmcl.2016.11.057. Epub 2016 Nov 22.


The role of regulator of G protein signaling 4 in delta-opioid receptor-mediated behaviors.

Dripps IJ, Wang Q, Neubig RR, Rice KC, Traynor JR, Jutkiewicz EM.

Psychopharmacology (Berl). 2017 Jan;234(1):29-39. doi: 10.1007/s00213-016-4432-5. Epub 2016 Sep 13.


Effects of N-Substitutions on the Tetrahydroquinoline (THQ) Core of Mixed-Efficacy μ-Opioid Receptor (MOR)/δ-Opioid Receptor (DOR) Ligands.

Harland AA, Bender AM, Griggs NW, Gao C, Anand JP, Pogozheva ID, Traynor JR, Jutkiewicz EM, Mosberg HI.

J Med Chem. 2016 May 26;59(10):4985-98. doi: 10.1021/acs.jmedchem.6b00308. Epub 2016 May 16.


Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.

Bender AM, Griggs NW, Gao C, Trask TJ, Traynor JR, Mosberg HI.

ACS Med Chem Lett. 2015 Oct 19;6(12):1199-203. doi: 10.1021/acsmedchemlett.5b00344. eCollection 2015 Dec 10.


Dynamic Coupling and Allosteric Networks in the α Subunit of Heterotrimeric G Proteins.

Yao XQ, Malik RU, Griggs NW, Skjærven L, Traynor JR, Sivaramakrishnan S, Grant BJ.

J Biol Chem. 2016 Feb 26;291(9):4742-53. doi: 10.1074/jbc.M115.702605. Epub 2015 Dec 24.


Further Optimization and Evaluation of Bioavailable, Mixed-Efficacy μ-Opioid Receptor (MOR) Agonists/δ-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.

Harland AA, Yeomans L, Griggs NW, Anand JP, Pogozheva ID, Jutkiewicz EM, Traynor JR, Mosberg HI.

J Med Chem. 2015 Nov 25;58(22):8952-69. doi: 10.1021/acs.jmedchem.5b01270. Epub 2015 Nov 13.


Ligand-Based Discovery of a New Scaffold for Allosteric Modulation of the μ-Opioid Receptor.

Bisignano P, Burford NT, Shang Y, Marlow B, Livingston KE, Fenton AM, Rockwell K, Budenholzer L, Traynor JR, Gerritz SW, Alt A, Filizola M.

J Chem Inf Model. 2015 Sep 28;55(9):1836-43. doi: 10.1021/acs.jcim.5b00388. Epub 2015 Sep 15.


Structural insights into µ-opioid receptor activation.

Huang W, Manglik A, Venkatakrishnan AJ, Laeremans T, Feinberg EN, Sanborn AL, Kato HE, Livingston KE, Thorsen TS, Kling RC, Granier S, Gmeiner P, Husbands SM, Traynor JR, Weis WI, Steyaert J, Dror RO, Kobilka BK.

Nature. 2015 Aug 20;524(7565):315-21. doi: 10.1038/nature14886. Epub 2015 Aug 5.


Asymmetric synthesis and in vitro and in vivo activity of tetrahydroquinolines featuring a diverse set of polar substitutions at the 6 position as mixed-efficacy μ opioid receptor/δ opioid receptor ligands.

Bender AM, Griggs NW, Anand JP, Traynor JR, Jutkiewicz EM, Mosberg HI.

ACS Chem Neurosci. 2015 Aug 19;6(8):1428-35. doi: 10.1021/acschemneuro.5b00100. Epub 2015 May 13.


Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.

Burford NT, Livingston KE, Canals M, Ryan MR, Budenholzer LM, Han Y, Shang Y, Herbst JJ, O'Connell J, Banks M, Zhang L, Filizola M, Bassoni DL, Wehrman TS, Christopoulos A, Traynor JR, Gerritz SW, Alt A.

J Med Chem. 2015 May 28;58(10):4220-9. doi: 10.1021/acs.jmedchem.5b00007. Epub 2015 May 7.


C7β-methyl analogues of the orvinols: the discovery of kappa opioid antagonists with nociceptin/orphanin FQ peptide (NOP) receptor partial agonism and low, or zero, efficacy at mu opioid receptors.

Cueva JP, Roche C, Ostovar M, Kumar V, Clark MJ, Hillhouse TM, Lewis JW, Traynor JR, Husbands SM.

J Med Chem. 2015 May 28;58(10):4242-9. doi: 10.1021/acs.jmedchem.5b00130. Epub 2015 May 6.


Selectivity and anti-Parkinson's potential of thiadiazolidinone RGS4 inhibitors.

Blazer LL, Storaska AJ, Jutkiewicz EM, Turner EM, Calcagno M, Wade SM, Wang Q, Huang XP, Traynor JR, Husbands SM, Morari M, Neubig RR.

ACS Chem Neurosci. 2015 Jun 17;6(6):911-9. doi: 10.1021/acschemneuro.5b00063. Epub 2015 Apr 20.


Themed section.

Christie MJ, Connor M, Traynor JR.

Br J Pharmacol. 2015 Jan;172(2):247-50. doi: 10.1111/bph.13028. No abstract available.


Disruption of the Na+ ion binding site as a mechanism for positive allosteric modulation of the mu-opioid receptor.

Livingston KE, Traynor JR.

Proc Natl Acad Sci U S A. 2014 Dec 23;111(51):18369-74. doi: 10.1073/pnas.1415013111. Epub 2014 Dec 8.


Nucleus accumbens shell excitability is decreased by methamphetamine self-administration and increased by 5-HT2C receptor inverse agonism and agonism.

Graves SM, Clark MJ, Traynor JR, Hu XT, Napier TC.

Neuropharmacology. 2015 Feb;89:113-21. doi: 10.1016/j.neuropharm.2014.09.001. Epub 2014 Sep 16.


Exploring pharmacological activities and signaling of morphinans substituted in position 6 as potent agonists interacting with the μ opioid receptor.

Ben Haddou T, Malfacini D, Calo G, Aceto MD, Harris LS, Traynor JR, Coop A, Schmidhammer H, Spetea M.

Mol Pain. 2014 Jul 24;10:48. doi: 10.1186/1744-8069-10-48.


Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.

Kumar V, Clark MJ, Traynor JR, Lewis JW, Husbands SM.

Bioorg Med Chem. 2014 Aug 1;22(15):4067-72. doi: 10.1016/j.bmc.2014.05.065. Epub 2014 Jun 12.


5-HT1A receptor-mediated phosphorylation of extracellular signal-regulated kinases (ERK1/2) is modulated by regulator of G protein signaling protein 19.

Wang Q, Terauchi A, Yee CH, Umemori H, Traynor JR.

Cell Signal. 2014 Sep;26(9):1846-52. doi: 10.1016/j.cellsig.2014.04.017. Epub 2014 May 2.


Selectively promiscuous opioid ligands: discovery of high affinity/low efficacy opioid ligands with substantial nociceptin opioid peptide receptor affinity.

Kumar V, Ridzwan IE, Grivas K, Lewis JW, Clark MJ, Meurice C, Jimenez-Gomez C, Pogozheva I, Mosberg H, Traynor JR, Husbands SM.

J Med Chem. 2014 May 22;57(10):4049-57. doi: 10.1021/jm401964y. Epub 2014 May 9.


Development of a bioavailable μ opioid receptor (MOPr) agonist, δ opioid receptor (DOPr) antagonist peptide that evokes antinociception without development of acute tolerance.

Mosberg HI, Yeomans L, Anand JP, Porter V, Sobczyk-Kojiro K, Traynor JR, Jutkiewicz EM.

J Med Chem. 2014 Apr 10;57(7):3148-53. doi: 10.1021/jm5002088. Epub 2014 Mar 26.


Challenges for opioid receptor nomenclature: IUPHAR Review 9.

Cox BM, Christie MJ, Devi L, Toll L, Traynor JR.

Br J Pharmacol. 2015 Jan;172(2):317-23. doi: 10.1111/bph.12612. Epub 2014 Jul 1. Review.


The Concise Guide to PHARMACOLOGY 2013/14: overview.

Alexander SP, Benson HE, Faccenda E, Pawson AJ, Sharman JL, McGrath JC, Catterall WA, Spedding M, Peters JA, Harmar AJ; CGTP Collaborators, Abul-Hasn N, Anderson CM, Anderson CM, Araiksinen MS, Arita M, Arthofer E, Barker EL, Barratt C, Barnes NM, Bathgate R, Beart PM, Belelli D, Bennett AJ, Birdsall NJ, Boison D, Bonner TI, Brailsford L, Bröer S, Brown P, Calo G, Carter WG, Catterall WA, Chan SL, Chao MV, Chiang N, Christopoulos A, Chun JJ, Cidlowski J, Clapham DE, Cockcroft S, Connor MA, Cox HM, Cuthbert A, Dautzenberg FM, Davenport AP, Dawson PA, Dent G, Dijksterhuis JP, Dollery CT, Dolphin AC, Donowitz M, Dubocovich ML, Eiden L, Eidne K, Evans BA, Fabbro D, Fahlke C, Farndale R, Fitzgerald GA, Fong TM, Fowler CJ, Fry JR, Funk CD, Futerman AH, Ganapathy V, Gaisnier B, Gershengorn MA, Goldin A, Goldman ID, Gundlach AL, Hagenbuch B, Hales TG, Hammond JR, Hamon M, Hancox JC, Hauger RL, Hay DL, Hobbs AJ, Hollenberg MD, Holliday ND, Hoyer D, Hynes NA, Inui KI, Ishii S, Jacobson KA, Jarvis GE, Jarvis MF, Jensen R, Jones CE, Jones RL, Kaibuchi K, Kanai Y, Kennedy C, Kerr ID, Khan AA, Klienz MJ, Kukkonen JP, Lapoint JY, Leurs R, Lingueglia E, Lippiat J, Lolait SJ, Lummis SC, Lynch JW, MacEwan D, Maguire JJ, Marshall IL, May JM, McArdle CA, McGrath JC, Michel MC, Millar NS, Miller LJ, Mitolo V, Monk PN, Moore PK, Moorhouse AJ, Mouillac B, Murphy PM, Neubig RR, Neumaier J, Niesler B, Obaidat A, Offermanns S, Ohlstein E, Panaro MA, Parsons S, Pwrtwee RG, Petersen J, Pin JP, Poyner DR, Prigent S, Prossnitz ER, Pyne NJ, Pyne S, Quigley JG, Ramachandran R, Richelson EL, Roberts RE, Roskoski R, Ross RA, Roth M, Rudnick G, Ryan RM, Said SI, Schild L, Sanger GJ, Scholich K, Schousboe A, Schulte G, Schulz S, Serhan CN, Sexton PM, Sibley DR, Siegel JM, Singh G, Sitsapesan R, Smart TG, Smith DM, Soga T, Stahl A, Stewart G, Stoddart LA, Summers RJ, Thorens B, Thwaites DT, Toll L, Traynor JR, Usdin TB, Vandenberg RJ, Villalon C, Vore M, Waldman SA, Ward DT, Willars GB, Wonnacott SJ, Wright E, Ye RD, Yonezawa A, Zimmermann M.

Br J Pharmacol. 2013 Dec;170(8):1449-58. doi: 10.1111/bph.12444.


Positive allosteric modulators of the μ-opioid receptor: a novel approach for future pain medications.

Burford NT, Traynor JR, Alt A.

Br J Pharmacol. 2015 Jan;172(2):277-86. doi: 10.1111/bph.12599. Epub 2014 Jul 1. Review.


Translation of structure-activity relationships from cyclic mixed efficacy opioid peptides to linear analogues.

Anand JP, Porter-Barrus VR, Waldschmidt HV, Yeomans L, Pogozheva ID, Traynor JR, Mosberg HI.

Biopolymers. 2014 Jan;102(1):107-14. doi: 10.1002/bip.22437. Erratum in: Biopolymers. 2014 Sep;102(5):426.


Characterization of BU09059: a novel potent selective κ-receptor antagonist.

Casal-Dominguez JJ, Furkert D, Ostovar M, Teintang L, Clark MJ, Traynor JR, Husbands SM, Bailey SJ.

ACS Chem Neurosci. 2014 Mar 19;5(3):177-84. doi: 10.1021/cn4001507. Epub 2014 Jan 28.


Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.

Bender AM, Clark MJ, Agius MP, Traynor JR, Mosberg HI.

Bioorg Med Chem Lett. 2014 Jan 15;24(2):548-51. doi: 10.1016/j.bmcl.2013.12.021. Epub 2013 Dec 11.


Synergistic activity between the delta-opioid agonist SNC80 and amphetamine occurs via a glutamatergic NMDA-receptor dependent mechanism.

Bosse KE, Jutkiewicz EM, Schultz-Kuszak KN, Mabrouk OS, Kennedy RT, Gnegy ME, Traynor JR.

Neuropharmacology. 2014 Feb;77:19-27. doi: 10.1016/j.neuropharm.2013.08.027. Epub 2013 Sep 10.


Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor.

Burford NT, Clark MJ, Wehrman TS, Gerritz SW, Banks M, O'Connell J, Traynor JR, Alt A.

Proc Natl Acad Sci U S A. 2013 Jun 25;110(26):10830-5. doi: 10.1073/pnas.1300393110. Epub 2013 Jun 10.


Differential control of opioid antinociception to thermal stimuli in a knock-in mouse expressing regulator of G-protein signaling-insensitive Gαo protein.

Lamberts JT, Smith CE, Li MH, Ingram SL, Neubig RR, Traynor JR.

J Neurosci. 2013 Mar 6;33(10):4369-77. doi: 10.1523/JNEUROSCI.5470-12.2013.


Opioid receptor interacting proteins and the control of opioid signaling.

Lamberts JT, Traynor JR.

Curr Pharm Des. 2013;19(42):7333-47. Review.


Increased agonist affinity at the μ-opioid receptor induced by prolonged agonist exposure.

Birdsong WT, Arttamangkul S, Clark MJ, Cheng K, Rice KC, Traynor JR, Williams JT.

J Neurosci. 2013 Feb 27;33(9):4118-27. doi: 10.1523/JNEUROSCI.4187-12.2013.

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