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Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-Gi Complex Structures.

Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Johnston CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ.

Cell. 2020 Feb 20;180(4):655-665.e18. doi: 10.1016/j.cell.2020.01.008. Epub 2020 Jan 30.


Toward Directing Opioid Receptor Signaling to Refine Opioid Therapeutics.

Grim TW, Acevedo-Canabal A, Bohn LM.

Biol Psychiatry. 2020 Jan 1;87(1):15-21. doi: 10.1016/j.biopsych.2019.10.020. Epub 2019 Oct 31. Review.


Probing the CB1 Cannabinoid Receptor Binding Pocket with AM6538, a High-Affinity Irreversible Antagonist.

Laprairie RB, Vemuri K, Stahl EL, Korde A, Ho JH, Grim TW, Hua T, Wu Y, Stevens RC, Liu ZJ, Makriyannis A, Bohn LM.

Mol Pharmacol. 2019 Nov;96(5):619-628. doi: 10.1124/mol.119.116483. Epub 2019 Sep 12.


A G protein signaling-biased agonist at the μ-opioid receptor reverses morphine tolerance while preventing morphine withdrawal.

Grim TW, Schmid CL, Stahl EL, Pantouli F, Ho JH, Acevedo-Canabal A, Kennedy NM, Cameron MD, Bannister TD, Bohn LM.

Neuropsychopharmacology. 2020 Jan;45(2):416-425. doi: 10.1038/s41386-019-0491-8. Epub 2019 Aug 23.


Quantitating Ligand Bias Using the Competitive Model of Ligand Activity.

Stahl EL, Ehlert FJ, Bohn LM.

Methods Mol Biol. 2019;1957:235-247. doi: 10.1007/978-1-4939-9158-7_15.


Crystal Structure of the Human Cannabinoid Receptor CB2.

Li X, Hua T, Vemuri K, Ho JH, Wu Y, Wu L, Popov P, Benchama O, Zvonok N, Locke K, Qu L, Han GW, Iyer MR, Cinar R, Coffey NJ, Wang J, Wu M, Katritch V, Zhao S, Kunos G, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ.

Cell. 2019 Jan 24;176(3):459-467.e13. doi: 10.1016/j.cell.2018.12.011. Epub 2019 Jan 10.


Repurposing of a Nucleoside Scaffold from Adenosine Receptor Agonists to Opioid Receptor Antagonists.

Tosh DK, Ciancetta A, Mannes P, Warnick E, Janowsky A, Eshleman AJ, Gizewski E, Brust TF, Bohn LM, Auchampach JA, Gao ZG, Jacobson KA.

ACS Omega. 2018 Oct 31;3(10):12658-12678. doi: 10.1021/acsomega.8b01237. Epub 2018 Oct 4.


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.

J Med Chem. 2018 Oct 11;61(19):8895-8907. doi: 10.1021/acs.jmedchem.8b01136. Epub 2018 Sep 24.


The effect of quinine in two bottle choice procedures in C57BL6 mice: Opioid preference, somatic withdrawal, and pharmacokinetic outcomes.

Grim TW, Park SJ, Schmid CL, Laprairie RB, Cameron M, Bohn LM.

Drug Alcohol Depend. 2018 Oct 1;191:195-202. doi: 10.1016/j.drugalcdep.2018.05.034. Epub 2018 Aug 2.


Arrestin recruitment to dopamine D2 receptor mediates locomotion but not incentive motivation.

Donthamsetti P, Gallo EF, Buck DC, Stahl EL, Zhu Y, Lane JR, Bohn LM, Neve KA, Kellendonk C, Javitch JA.

Mol Psychiatry. 2018 Aug 17. doi: 10.1038/s41380-018-0212-4. [Epub ahead of print]


G protein signaling-biased agonism at the κ-opioid receptor is maintained in striatal neurons.

Ho JH, Stahl EL, Schmid CL, Scarry SM, Aubé J, Bohn LM.

Sci Signal. 2018 Aug 7;11(542). pii: eaar4309. doi: 10.1126/scisignal.aar4309.


O6C-20-nor-salvinorin A is a stable and potent KOR agonist.

Hirasawa S, Cho M, Brust TF, Roach JJ, Bohn LM, Shenvi RA.

Bioorg Med Chem Lett. 2018 Sep 1;28(16):2770-2772. doi: 10.1016/j.bmcl.2018.01.055. Epub 2018 Jan 31.


Dynamic Strategic Bond Analysis Yields a Ten-Step Synthesis of 20-nor-Salvinorin A, a Potent κ-OR Agonist.

Roach JJ, Sasano Y, Schmid CL, Zaidi S, Katritch V, Stevens RC, Bohn LM, Shenvi RA.

ACS Cent Sci. 2017 Dec 27;3(12):1329-1336. doi: 10.1021/acscentsci.7b00488. Epub 2017 Dec 13.


Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics.

Schmid CL, Kennedy NM, Ross NC, Lovell KM, Yue Z, Morgenweck J, Cameron MD, Bannister TD, Bohn LM.

Cell. 2017 Nov 16;171(5):1165-1175.e13. doi: 10.1016/j.cell.2017.10.035.


Approaches to Assess Biased Signaling at the CB1R Receptor.

Laprairie RB, Stahl EL, Bohn LM.

Methods Enzymol. 2017;593:259-279. doi: 10.1016/bs.mie.2017.06.031. Epub 2017 Jul 5.


Seeking (and Finding) Biased Ligands of the Kappa Opioid Receptor.

Bohn LM, Aubé J.

ACS Med Chem Lett. 2017 Jul 5;8(7):694-700. doi: 10.1021/acsmedchemlett.7b00224. eCollection 2017 Jul 13.


Crystal structures of agonist-bound human cannabinoid receptor CB1.

Hua T, Vemuri K, Nikas SP, Laprairie RB, Wu Y, Qu L, Pu M, Korde A, Jiang S, Ho JH, Han GW, Ding K, Li X, Liu H, Hanson MA, Zhao S, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ.

Nature. 2017 Jul 27;547(7664):468-471. doi: 10.1038/nature23272. Epub 2017 Jul 5.


Correction to "Structure-Activity Relationship Studies of Functionally Selective Kappa Opioid Receptor Agonists that Modulate ERK 1/2 Phosphorylation While Preserving G Protein Over βArrestin2 Signaling Bias".

Lovell KM, Frankowski KJ, Stahl EL, Slauson SR, Yoo E, Prisinzano TE, Aubé J, Bohn LM.

ACS Chem Neurosci. 2017 Jul 19;8(7):1628. doi: 10.1021/acschemneuro.7b00157. Epub 2017 May 25. No abstract available.


Stolonidiol: Synthesis, Target Identification, and Mechanism for Choline Acetyltransferase Activation.

Mason JW, Schmid CL, Bohn LM, Roush WR.

J Am Chem Soc. 2017 Apr 26;139(16):5865-5869. doi: 10.1021/jacs.7b01083. Epub 2017 Apr 17.


RasGRP1 promotes amphetamine-induced motor behavior through a Rhes interaction network ("Rhesactome") in the striatum.

Shahani N, Swarnkar S, Giovinazzo V, Morgenweck J, Bohn LM, Scharager-Tapia C, Pascal B, Martinez-Acedo P, Khare K, Subramaniam S.

Sci Signal. 2016 Nov 15;9(454):ra111.


Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria.

Brust TF, Morgenweck J, Kim SA, Rose JH, Locke JL, Schmid CL, Zhou L, Stahl EL, Cameron MD, Scarry SM, Aubé J, Jones SR, Martin TJ, Bohn LM.

Sci Signal. 2016 Nov 29;9(456):ra117.


Synthesis of Kappa Opioid Antagonists Based On Pyrrolo[1,2-α]quinoxalinones Using an N-Arylation/Condensation/Oxidation Reaction Sequence.

Scarry SM, Lovell KM, Frankowski KJ, Bohn LM, Aubé J.

J Org Chem. 2016 Nov 4;81(21):10538-10550. Epub 2016 Aug 2.


Crystal Structure of the Human Cannabinoid Receptor CB1.

Hua T, Vemuri K, Pu M, Qu L, Han GW, Wu Y, Zhao S, Shui W, Li S, Korde A, Laprairie RB, Stahl EL, Ho JH, Zvonok N, Zhou H, Kufareva I, Wu B, Zhao Q, Hanson MA, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ.

Cell. 2016 Oct 20;167(3):750-762.e14. doi: 10.1016/j.cell.2016.10.004.


Synthetic Ligands of Cannabinoid Receptors Affect Dauer Formation in the Nematode Caenorhabditis elegans.

Reis Rodrigues P, Kaul TK, Ho JH, Lucanic M, Burkewitz K, Mair WB, Held JM, Bohn LM, Gill MS.

G3 (Bethesda). 2016 Jun 1;6(6):1695-705. doi: 10.1534/g3.116.026997.


Biased agonism: An emerging paradigm in GPCR drug discovery.

Rankovic Z, Brust TF, Bohn LM.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):241-250. doi: 10.1016/j.bmcl.2015.12.024. Epub 2015 Dec 9. Review.


Recruitment of β-Arrestin into Neuronal Cilia Modulates Somatostatin Receptor Subtype 3 Ciliary Localization.

Green JA, Schmid CL, Bley E, Monsma PC, Brown A, Bohn LM, Mykytyn K.

Mol Cell Biol. 2015 Oct 26;36(1):223-35. doi: 10.1128/MCB.00765-15. Print 2016 Jan 1.


5-HT1A Autoreceptors in the Dorsal Raphe Nucleus Convey Vulnerability to Compulsive Cocaine Seeking.

You IJ, Wright SR, Garcia-Garcia AL, Tapper AR, Gardner PD, Koob GF, David Leonardo E, Bohn LM, Wee S.

Neuropsychopharmacology. 2016 Apr;41(5):1210-22. doi: 10.1038/npp.2015.268. Epub 2015 Sep 1.


Investigation of the role of βarrestin2 in kappa opioid receptor modulation in a mouse model of pruritus.

Morgenweck J, Frankowski KJ, Prisinzano TE, Aubé J, Bohn LM.

Neuropharmacology. 2015 Dec;99:600-9. doi: 10.1016/j.neuropharm.2015.08.027. Epub 2015 Aug 25.


Approaches to Assess Functional Selectivity in GPCRs: Evaluating G Protein Signaling in an Endogenous Environment.

Bohn LM, Zhou L, Ho JH.

Methods Mol Biol. 2015;1335:177-89. doi: 10.1007/978-1-4939-2914-6_12.


Exploring the Biology of G Protein-Coupled Receptors from In Vitro to In Vivo.

Bohn LM, Lohse MJ, Nitabach MN, Taghert PH, Smit MJ.

Mol Pharmacol. 2015 Sep;88(3):534-5. doi: 10.1124/mol.115.100750. Epub 2015 Jul 10.


Characterization of kappa opioid receptor mediated, dynorphin-stimulated [35S]GTPγS binding in mouse striatum for the evaluation of selective KOR ligands in an endogenous setting.

Zhou L, Stahl EL, Lovell KM, Frankowski KJ, Prisinzano TE, Aubé J, Bohn LM.

Neuropharmacology. 2015 Dec;99:131-41. doi: 10.1016/j.neuropharm.2015.07.001. Epub 2015 Jul 6.


Fulfilling the Promise of "Biased" G Protein-Coupled Receptor Agonism.

Luttrell LM, Maudsley S, Bohn LM.

Mol Pharmacol. 2015 Sep;88(3):579-88. doi: 10.1124/mol.115.099630. Epub 2015 Jul 1. Review.


Molecular-interaction and signaling profiles of AM3677, a novel covalent agonist selective for the cannabinoid 1 receptor.

Janero DR, Yaddanapudi S, Zvonok N, Subramanian KV, Shukla VG, Stahl E, Zhou L, Hurst D, Wager-Miller J, Bohn LM, Reggio PH, Mackie K, Makriyannis A.

ACS Chem Neurosci. 2015 Aug 19;6(8):1400-10. doi: 10.1021/acschemneuro.5b00090. Epub 2015 May 29.


Structure-activity relationship studies of functionally selective kappa opioid receptor agonists that modulate ERK 1/2 phosphorylation while preserving G protein over βarrestin2 signaling bias.

Lovell KM, Frankowski KJ, Stahl EL, Slauson SR, Yoo E, Prisinzano TE, Aubé J, Bohn LM.

ACS Chem Neurosci. 2015 Aug 19;6(8):1411-9. doi: 10.1021/acschemneuro.5b00092. Epub 2015 May 1. Erratum in: ACS Chem Neurosci. 2017 Jul 19;8(7):1628.


A novel method for analyzing extremely biased agonism at G protein-coupled receptors.

Stahl EL, Zhou L, Ehlert FJ, Bohn LM.

Mol Pharmacol. 2015 May;87(5):866-77. doi: 10.1124/mol.114.096503. Epub 2015 Feb 13.


Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.

Frankowski KJ, Slauson SR, Lovell KM, Phillips AM, Streicher JM, Zhou L, Whipple DA, Schoenen FJ, Prisinzano TE, Bohn LM, Aubé J.

Bioorg Med Chem. 2015 Jul 15;23(14):3948-56. doi: 10.1016/j.bmc.2014.12.033. Epub 2014 Dec 23.


Functional selectivity of GPCR signaling in animals.

Zhou L, Bohn LM.

Curr Opin Cell Biol. 2014 Apr;27:102-8. doi: 10.1016/ Epub 2013 Dec 22. Review.


Clozapine acts as an agonist at serotonin 2A receptors to counter MK-801-induced behaviors through a βarrestin2-independent activation of Akt.

Schmid CL, Streicher JM, Meltzer HY, Bohn LM.

Neuropsychopharmacology. 2014 Jul;39(8):1902-13. doi: 10.1038/npp.2014.38. Epub 2014 Feb 17.


β-arrestins: regulatory role and therapeutic potential in opioid and cannabinoid receptor-mediated analgesia.

Raehal KM, Bohn LM.

Handb Exp Pharmacol. 2014;219:427-43. doi: 10.1007/978-3-642-41199-1_22. Review.


Development of functionally selective, small molecule agonists at kappa opioid receptors.

Zhou L, Lovell KM, Frankowski KJ, Slauson SR, Phillips AM, Streicher JM, Stahl E, Schmid CL, Hodder P, Madoux F, Cameron MD, Prisinzano TE, Aubé J, Bohn LM.

J Biol Chem. 2013 Dec 20;288(51):36703-16. doi: 10.1074/jbc.M113.504381. Epub 2013 Nov 1.


Functional selectivity of 6'-guanidinonaltrindole (6'-GNTI) at κ-opioid receptors in striatal neurons.

Schmid CL, Streicher JM, Groer CE, Munro TA, Zhou L, Bohn LM.

J Biol Chem. 2013 Aug 2;288(31):22387-98. doi: 10.1074/jbc.M113.476234. Epub 2013 Jun 17.


GIRK channel modulation by assembly with allosterically regulated RGS proteins.

Zhou H, Chisari M, Raehal KM, Kaltenbronn KM, Bohn LM, Mennerick SJ, Blumer KJ.

Proc Natl Acad Sci U S A. 2012 Dec 4;109(49):19977-82. doi: 10.1073/pnas.1214337109. Epub 2012 Nov 19.


Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.

Frankowski KJ, Hedrick MP, Gosalia P, Li K, Shi S, Whipple D, Ghosh P, Prisinzano TE, Schoenen FJ, Su Y, Vasile S, Sergienko E, Gray W, Hariharan S, Milan L, Heynen-Genel S, Mangravita-Novo A, Vicchiarelli M, Smith LH, Streicher JM, Caron MG, Barak LS, Bohn LM, Chung TD, Aubé J.

ACS Chem Neurosci. 2012 Mar 21;3(3):221-236. Epub 2012 Jan 20.


β-arrestin2 regulates cannabinoid CB1 receptor signaling and adaptation in a central nervous system region-dependent manner.

Nguyen PT, Schmid CL, Raehal KM, Selley DE, Bohn LM, Sim-Selley LJ.

Biol Psychiatry. 2012 Apr 15;71(8):714-24. doi: 10.1016/j.biopsych.2011.11.027. Epub 2012 Jan 20.


Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.

Béguin C, Potuzak J, Xu W, Liu-Chen LY, Streicher JM, Groer CE, Bohn LM, Carlezon WA Jr, Cohen BM.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1023-6. doi: 10.1016/j.bmcl.2011.11.128. Epub 2011 Dec 7.


Antinociceptive effects of herkinorin, a MOP receptor agonist derived from salvinorin A in the formalin test in rats: new concepts in mu opioid receptor pharmacology: from a symposium on new concepts in mu-opioid pharmacology.

Lamb K, Tidgewell K, Simpson DS, Bohn LM, Prisinzano TE.

Drug Alcohol Depend. 2012 Mar 1;121(3):181-8. doi: 10.1016/j.drugalcdep.2011.10.026. Epub 2011 Nov 26.


Antagonist for the Kappa Opioid Receptor.

Hedrick MP, Gosalia P, Li K, Frankowski KJ, Shi S, Prisinzano TE, Schoenen F, Aubé J, Su Y, Stonich D, Vasile S, Sergienko E, Gray W, Hariharan S, Milan L, Heynen-Genel S, Vicchiarelli M, Mangravita-Novo A, Streicher JM, Smith LH, Chung TDY, Caron M, Bohn LM, Barak LS.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Oct 31 [updated 2011 May 26].


Functional selectivity at the μ-opioid receptor: implications for understanding opioid analgesia and tolerance.

Raehal KM, Schmid CL, Groer CE, Bohn LM.

Pharmacol Rev. 2011 Dec;63(4):1001-19. doi: 10.1124/pr.111.004598. Epub 2011 Aug 26. Review.


Agonist-directed interactions with specific beta-arrestins determine mu-opioid receptor trafficking, ubiquitination, and dephosphorylation.

Groer CE, Schmid CL, Jaeger AM, Bohn LM.

J Biol Chem. 2011 Sep 9;286(36):31731-41. doi: 10.1074/jbc.M111.248310. Epub 2011 Jul 14.


Synthesis of conolidine, a potent non-opioid analgesic for tonic and persistent pain.

Tarselli MA, Raehal KM, Brasher AK, Streicher JM, Groer CE, Cameron MD, Bohn LM, Micalizio GC.

Nat Chem. 2011 Jun;3(6):449-53. doi: 10.1038/nchem.1050.


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