Recent Publications

Recent Publications

Nitro-benzylideneoxymorphone, a bifunctional mu and delta opioid receptor ligand with high mu opioid receptor efficacy.

Olson KM, Devereaux AL, Chatterjee P, Saldaña-Shumaker SL, Shafer A, Plotkin A, Kandasamy R, MacKerell AD Jr, Traynor JR, Cunningham CW.

Front Pharmacol. 2023 Jul 3;14:1230053. doi: 10.3389/fphar.2023.1230053. eCollection 2023.

PMID: 37469877.

Application of Mixed-Solvent Molecular Dynamics Simulations for Prediction of Allosteric Sites on G Protein-Coupled Receptors.

Chan WKB, Carlson HA, Traynor JR.

Mol Pharmacol. 2023 May;103(5):274-285. doi: 10.1124/molpharm.122.000612. Epub 2023 Mar 3.

PMID: 36868791

Opioid research in the time of the opioid crisis.

Traynor JR, Moron JA.

Br J Pharmacol. 2023 Apr;180(7):793-796. doi: 10.1111/bph.16043. Epub 2023 Feb 22.

PMID: 36813266

PACAP and acetylcholine cause distinct Ca2+ signals and secretory responses in chromaffin cells.

Morales A, Mohan R, Chen X, Coffman BL, Bendahmane M, Watch L, West JL, Bakshi S, Traynor JR, Giovannucci DR, Kammermeier PJ, Axelrod D, Currie KPM, Smrcka AV, Anantharam A.

J Gen Physiol. 2023 Feb 6;155(2):e202213180. doi: 10.1085/jgp.202213180. Epub 2022 Dec 20.

PMID: 36538657.

Delta Opioid Receptor-Mediated Antidepressant-Like Effects of Diprenorphine in Mice.

Olson KM, Hillhouse TM, Burgess GE, West JL, Hallahan JE, Dripps IJ, Ladetto AG, Rice KC, Jutkiewicz EM, Traynor JR.

J Pharmacol Exp Ther. 2023 Mar;384(3):343-352. doi: 10.1124/jpet.122.001182. Epub 2022 Dec 1.

PMID: 36456196 

Opioid Antagonists from the Orvinol Series as Potential Reversal Agents for Opioid Overdose.

Disney A, Olson KM, Shafer AM, Moore SC, Anand JP, Traynor JR, Husbands SM.

ACS Chem Neurosci. 2022 Nov 2;13(21):3108-3117. doi: 10.1021/acschemneuro.2c00464. Epub 2022 Oct 12.

PMID: 36223082

Finding the Perfect Fit: Conformational Biosensors to Determine the Efficacy of GPCR Ligands.

Olson KM, Campbell A, Alt A, Traynor JR.

ACS Pharmacol Transl Sci. 2022 Aug 14;5(9):694-709. doi: 10.1021/acsptsci.1c00256. eCollection 2022 Sep 9.

PMID: 36110374 

OREX-1038: a potential new treatment for pain with low abuse liability and limited adverse effects.

Gerak LR, Maguire DR, Cami-Kobeci G, Olson KM, Traynor JR, Husbands SM, France CP, Acevedo L, Belli B, Flynn P.

Behav Pharmacol. 2022 Sep 1;33(6):377-394. doi: 10.1097/FBP.0000000000000684. Epub 2022 Aug 3.

PMID: 35947066 

In silico analysis of SARS-CoV-2 proteins as targets for clinically available drugs.

Chan WKB, Olson KM, Wotring JW, Sexton JZ, Carlson HA, Traynor JR.

Sci Rep. 2022 Mar 29;12(1):5320. doi: 10.1038/s41598-022-08320-y.

PMID: 35351926.

Allosteric Modulator Leads Hiding in Plain Site: Developing Peptide and Peptidomimetics as GPCR Allosteric Modulators.

Olson KM, Traynor JR, Alt A.

Front Chem. 2021 Oct 7;9:671483. doi: 10.3389/fchem.2021.671483. eCollection 2021.

PMID: 34692635       

Mixed-solvent molecular dynamics simulation-based discovery of a putative allosteric site on regulator of G protein signaling 4.

Chan WKB, DasGupta D, Carlson HA, Traynor JR.

J Comput Chem. 2021 Nov 15;42(30):2170-2180. doi: 10.1002/jcc.26747. Epub 2021 Sep 7.

PMID: 34494289.

Reply to Zhuang et al.: Potential side effects of positive allosteric modulators of the mu-opioid receptor.

Traynor JR.

Proc Natl Acad Sci U S A. 2021 Jul 13;118(28):e2108493118. doi: 10.1073/pnas.2108493118.

PMID: 34260391 

The Buprenorphine Analogue BU10119 Attenuates Drug-Primed and Stress-Induced Cocaine Reinstatement in Mice.

Hillhouse TM, Olson KM, Hallahan JE, Rysztak LG, Sears BF, Meurice C, Ostovar M, Koppenhaver PO, West JL, Jutkiewicz EM, Husbands SM, Traynor JR.

J Pharmacol Exp Ther. 2021 Sep;378(3):287-299. doi: 10.1124/jpet.121.000524. Epub 2021 Jun 28.

PMID: 34183434

Mice Expressing Regulators of G protein Signaling-insensitive Gαo Define Roles of μ Opioid Receptor Gαo and Gαi Subunit Coupling in Inhibition of Presynaptic GABA Release.

Bouchet CA, McPherson KB, Li MH, Traynor JR, Ingram SL.

Mol Pharmacol. 2021 Sep;100(3):217-223. doi: 10.1124/molpharm.121.000249. Epub 2021 Jun 16.

PMID: 34135098 

Positive allosteric modulation of the mu-opioid receptor produces analgesia with reduced side effects.

Kandasamy R, Hillhouse TM, Livingston KE, Kochan KE, Meurice C, Eans SO, Li MH, White AD, Roques BP, McLaughlin JP, Ingram SL, Burford NT, Alt A, Traynor JR.

Proc Natl Acad Sci U S A. 2021 Apr 20;118(16):e2000017118. doi: 10.1073/pnas.2000017118.

PMID: 33846240 

SAR Matrices Enable Discovery of Mixed Efficacy μ-Opioid Receptor Agonist Peptidomimetics with Simplified Structures through an Aromatic-Amine Pharmacophore.

Henry S, Anand JP, Brinkel AC, McMillan DM, Twarozynski JJ, Loo CE, Traynor JR, Mosberg HI.

ACS Chem Neurosci. 2021 Jan 6;12(1):216-233. doi: 10.1021/acschemneuro.0c00693. Epub 2020 Dec 21.

PMID: 33346631 

Author Correction: 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. 2020 Aug;584(7820):E16. doi: 10.1038/s41586-020-2542-z.

PMID: 32724208

The Intriguing Effects of Substituents in the N-Phenethyl Moiety of Norhydromorphone: A Bifunctional Opioid from a Set of "Tail Wags Dog" Experiments.

Wang M, Irvin TC, Herdman CA, Hanna RD, Hassan SA, Lee YS, Kaska S, Crowley RS, Prisinzano TE, Withey SL, Paronis CA, Bergman J, Inan S, Geller EB, Adler MW, Kopajtic TA, Katz JL, Chadderdon AM, Traynor JR, Jacobson AE, Rice KC.

Molecules. 2020 Jun 6;25(11):2640. doi: 10.3390/molecules25112640.

PMID: 32517185 

Pharmacological Properties of δ-Opioid Receptor-Mediated Behaviors: Agonist Efficacy and Receptor Reserve.

Dripps IJ, Chen R, Shafer AM, Livingston KE, Disney A, Husbands SM, Traynor JR, Rice KC, Jutkiewicz EM.

J Pharmacol Exp Ther. 2020 Aug;374(2):319-330. doi: 10.1124/jpet.119.262717. Epub 2020 May 28.

PMID: 32467352 

In vitro pharmacology of fentanyl analogs at the human mu opioid receptor and their spectroscopic analysis.

Hassanien SH, Bassman JR, Perrien Naccarato CM, Twarozynski JJ, Traynor JR, Iula DM, Anand JP.

Drug Test Anal. 2020 Aug;12(8):1212-1221. doi: 10.1002/dta.2822. Epub 2020 Jun 11.

PMID: 32415719 

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.

PMID: 32038168  

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.

PMID: 31986033 

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):4302. doi: 10.3390/molecules24234302.

PMID: 31779072 

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.

PMID: 31199621

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.

PMID: 30924650 

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.

PMID: 30916966 

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.

PMID: 30710458 

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.

PMID: 30483131 

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.

PMID: 30189184 

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.

PMID: 30150362 

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.

PMID: 29932421

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. PMID: 29677442

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. PMID: 29352503

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. PMID: 29278419

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. PMID: 29233847

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. PMID: 28971229

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. PMID: 28796483

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.

PMID: 28419415

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. PMID: 28314512

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. PMID: 28011222

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. PMID: 27624599

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. PMID: 27148755

Contact Information: Dr. John Traynor | Email: jtraynor@umich.edu | Phone: 734.647.7479 | Fax: 734.763.4450