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Items: 1 to 50 of 81

1.

Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7.

Lamb KN, Bsteh D, Dishman SN, Moussa HF, Fan H, Stuckey JI, Norris JL, Cholensky SH, Li D, Wang J, Sagum C, Stanton BZ, Bedford MT, Pearce KH, Kenakin TP, Kireev DB, Wang GG, James LI, Bell O, Frye SV.

Cell Chem Biol. 2019 Oct 17;26(10):1365-1379.e22. doi: 10.1016/j.chembiol.2019.07.013. Epub 2019 Aug 15.

PMID:
31422906

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2.

Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68).

Yu X, Huang XP, Kenakin TP, Slocum ST, Chen X, Martini ML, Liu J, Jin J.

J Med Chem. 2019 Aug 22;62(16):7557-7574. doi: 10.1021/acs.jmedchem.9b00869. Epub 2019 Aug 1.

PMID:
31298539

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3.

Diarylureas Containing 5-Membered Heterocycles as CB1 Receptor Allosteric Modulators: Design, Synthesis, and Pharmacological Evaluation.

Nguyen T, Gamage TF, Decker AM, German N, Langston TL, Farquhar CE, Kenakin TP, Wiley JL, Thomas BF, Zhang Y.

ACS Chem Neurosci. 2019 Jan 16;10(1):518-527. doi: 10.1021/acschemneuro.8b00396. Epub 2018 Sep 20.

PMID:
30188693

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4.

Neutrophil priming that turns natural FFA2R agonists into potent activators of the superoxide generating NADPH-oxidase.

Mårtensson J, Holdfeldt A, Sundqvist M, Gabl M, Kenakin TP, Björkman L, Forsman H, Dahlgren C.

J Leukoc Biol. 2018 Dec;104(6):1117-1132. doi: 10.1002/JLB.2A0318-130RR. Epub 2018 Aug 22.

PMID:
30134499

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5.

Editors in Chief Overview.

Trist DG, Kenakin TP.

Curr Opin Pharmacol. 2017 Aug;35:iv-v. doi: 10.1016/j.coph.2017.11.003. No abstract available.

PMID:
29241830

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6.

In memory of Norman Bowery (1944-2016).

Trist DG, Kenakin TP, Blackburn TP.

Curr Opin Pharmacol. 2017 Aug;35:89-93. doi: 10.1016/j.coph.2017.05.008. Epub 2017 Aug 29.

PMID:
28864032

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7.

Detailed Characterization of the In Vitro Pharmacological and Pharmacokinetic Properties of N-(2-Hydroxybenzyl)-2,5-Dimethoxy-4-Cyanophenylethylamine (25CN-NBOH), a Highly Selective and Brain-Penetrant 5-HT2A Receptor Agonist.

Jensen AA, McCorvy JD, Leth-Petersen S, Bundgaard C, Liebscher G, Kenakin TP, Bräuner-Osborne H, Kehler J, Kristensen JL.

J Pharmacol Exp Ther. 2017 Jun;361(3):441-453. doi: 10.1124/jpet.117.239905. Epub 2017 Mar 30.

PMID:
28360333

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8.

Identification of the first biased NPS receptor agonist that retains anxiolytic and memory promoting effects with reduced levels of locomotor stimulation.

Clark SD, Kenakin TP, Gertz S, Hassler C, Gay EA, Langston TL, Reinscheid RK, Runyon SP.

Neuropharmacology. 2017 May 15;118:69-78. doi: 10.1016/j.neuropharm.2017.03.001. Epub 2017 Mar 3.

PMID:
28267583
Free PMC Article

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9.

Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor.

Laprairie RB, Kulkarni PM, Deschamps JR, Kelly MEM, Janero DR, Cascio MG, Stevenson LA, Pertwee RG, Kenakin TP, Denovan-Wright EM, Thakur GA.

ACS Chem Neurosci. 2017 Jun 21;8(6):1188-1203. doi: 10.1021/acschemneuro.6b00310. Epub 2017 Feb 7.

PMID:
28103441

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10.

Allosteric Modulation: An Alternate Approach Targeting the Cannabinoid CB1 Receptor.

Nguyen T, Li JX, Thomas BF, Wiley JL, Kenakin TP, Zhang Y.

Med Res Rev. 2017 May;37(3):441-474. doi: 10.1002/med.21418. Epub 2016 Nov 23. Review.

PMID:
27879006
Free PMC Article

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11.

Human native kappa opioid receptor functions not predicted by recombinant receptors: Implications for drug design.

Broad J, Maurel D, Kung VW, Hicks GA, Schemann M, Barnes MR, Kenakin TP, Granier S, Sanger GJ.

Sci Rep. 2016 Aug 5;6:30797. doi: 10.1038/srep30797.

PMID:
27492592
Free PMC Article

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12.

Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.

Davoren JE, Lee CW, Garnsey M, Brodney MA, Cordes J, Dlugolenski K, Edgerton JR, Harris AR, Helal CJ, Jenkinson S, Kauffman GW, Kenakin TP, Lazzaro JT, Lotarski SM, Mao Y, Nason DM, Northcott C, Nottebaum L, O'Neil SV, Pettersen B, Popiolek M, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Zhang L, Grimwood S.

J Med Chem. 2016 Jul 14;59(13):6313-28. doi: 10.1021/acs.jmedchem.6b00544. Epub 2016 Jul 1.

PMID:
27275946

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13.

Synoptic pharmacology: Detecting and assessing the pharmacological significance of ligands for orphan receptors.

Kenakin TP.

Pharmacol Res. 2016 Dec;114:284-290. doi: 10.1016/j.phrs.2016.01.022. Epub 2016 Jan 21. Review.

PMID:
26804250

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14.

Structure-activity relationships of substituted 1H-indole-2-carboxamides as CB1 receptor allosteric modulators.

Nguyen T, German N, Decker AM, Li JX, Wiley JL, Thomas BF, Kenakin TP, Zhang Y.

Bioorg Med Chem. 2015 May 1;23(9):2195-2203. doi: 10.1016/j.bmc.2015.02.058. Epub 2015 Mar 7.

PMID:
25797163
Free PMC Article

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15.

International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric ligands.

Christopoulos A, Changeux JP, Catterall WA, Fabbro D, Burris TP, Cidlowski JA, Olsen RW, Peters JA, Neubig RR, Pin JP, Sexton PM, Kenakin TP, Ehlert FJ, Spedding M, Langmead CJ.

Pharmacol Rev. 2014 Oct;66(4):918-47. doi: 10.1124/pr.114.008862.

PMID:
25026896

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16.

Biased signalling and allosteric machines: new vistas and challenges for drug discovery.

Kenakin TP.

Br J Pharmacol. 2012 Mar;165(6):1659-1669. doi: 10.1111/j.1476-5381.2011.01749.x. Review.

PMID:
22023017
Free PMC Article

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17.

Refining efficacy: allosterism and bias in G protein-coupled receptor signaling.

Luttrell LM, Kenakin TP.

Methods Mol Biol. 2011;756:3-35. doi: 10.1007/978-1-61779-160-4_1. Review.

PMID:
21870218

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18.

Journal of Receptors and Signal Transduction. Editorial.

Eberle AN, Kenakin TP.

J Recept Signal Transduct Res. 2010 Dec;30(6):371. doi: 10.3109/10799893.2010.532383. No abstract available.

PMID:
21105854

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19.

Ligand detection in the allosteric world.

Kenakin TP.

J Biomol Screen. 2010 Feb;15(2):119-30. doi: 10.1177/1087057109357789. Epub 2010 Jan 19. Review.

PMID:
20086210

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20.

'7TM receptor allostery: putting numbers to shapeshifting proteins.

Kenakin TP.

Trends Pharmacol Sci. 2009 Sep;30(9):460-9. doi: 10.1016/j.tips.2009.06.007. Epub 2009 Sep 2. Review.

PMID:
19729207

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21.

Cellular assays as portals to seven-transmembrane receptor-based drug discovery.

Kenakin TP.

Nat Rev Drug Discov. 2009 Aug;8(8):617-26. doi: 10.1038/nrd2838. Epub 2009 Jul 17. Review.

PMID:
19609267

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22.

The relative activity of "function sparing" HIV-1 entry inhibitors on viral entry and CCR5 internalization: is allosteric functional selectivity a valuable therapeutic property?

Muniz-Medina VM, Jones S, Maglich JM, Galardi C, Hollingsworth RE, Kazmierski WM, Ferris RG, Edelstein MP, Chiswell KE, Kenakin TP.

Mol Pharmacol. 2009 Mar;75(3):490-501. doi: 10.1124/mol.108.052555. Epub 2008 Dec 8.

PMID:
19064629

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23.

Seven transmembrane receptors as nature's prototype allosteric protein: de-emphasizing the geography of binding.

Kenakin TP.

Mol Pharmacol. 2008 Sep;74(3):541-3. doi: 10.1124/mol.108.050062. Epub 2008 Jun 26.

PMID:
18583453

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24.

Pharmacological onomastics: what's in a name?

Kenakin TP.

Br J Pharmacol. 2008 Feb;153(3):432-8. Epub 2007 Aug 13. Review.

PMID:
17700724
Free PMC Article

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25.

Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.

Briscoe CP, Peat AJ, McKeown SC, Corbett DF, Goetz AS, Littleton TR, McCoy DC, Kenakin TP, Andrews JL, Ammala C, Fornwald JA, Ignar DM, Jenkinson S.

Br J Pharmacol. 2006 Jul;148(5):619-28. Epub 2006 May 15.

PMID:
16702987
Free PMC Article

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26.

Peptide, peptidomimetic and small-molecule drug discovery targeting HIV-1 host-cell attachment and entry through gp120, gp41, CCR5 and CXCR4.

Kazmierski WM, Kenakin TP, Gudmundsson KS.

Chem Biol Drug Des. 2006 Jan;67(1):13-26. Review.

PMID:
16492145

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27.

New eyes to see texture in ligand efficacy.

Kenakin TP.

Nat Methods. 2005 Mar;2(3):163-4. No abstract available.

PMID:
15782182

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28.

The secret lives of GPCRs.

Kenakin TP.

Drug Discov Today. 2003 Aug 1;8(15):674. No abstract available.

PMID:
12927508

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29.

Quantitation in receptor pharmacology.

Kenakin TP.

Receptors Channels. 2001;7(5):371-85.

PMID:
11697080

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30.

Uncovering biases in high throughput screens of G-protein coupled receptors.

Woolf PJ, Kenakin TP, Linderman JJ.

J Theor Biol. 2001 Feb 21;208(4):403-18.

PMID:
11222046

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31.

Protean effects of a natural peptide agonist of the G protein-coupled secretin receptor demonstrated by receptor mutagenesis.

Ganguli SC, Park CG, Holtmann MH, Hadac EM, Kenakin TP, Miller LJ.

J Pharmacol Exp Ther. 1998 Aug;286(2):593-8.

PMID:
9694908

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32.

A mathematical model for analysis of pharmacologically induced changes in the kinetics of cardiac muscle.

Lutz MW, Morgan PH, Kenakin TP, Goetz A, Queen K, Irving P, Rose D, Gill JM, Rimele T.

J Pharmacol Toxicol Methods. 1996 Nov;36(3):171-83.

PMID:
8959583

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33.

The cubic ternary complex receptor-occupancy model. III. resurrecting efficacy.

Weiss JM, Morgan PH, Lutz MW, Kenakin TP.

J Theor Biol. 1996 Aug 21;181(4):381-97.

PMID:
8949584

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34.

Use of resampling techniques to estimate the variance of parameters in pharmacological assays when experimental protocols preclude independent replication: an example using Schild regressions.

Lutz MW, Kenakin TP, Corsi M, Menius JA, Krishnamoorthy C, Rimele T, Morgan PH.

J Pharmacol Toxicol Methods. 1995 Sep;34(1):37-46.

PMID:
7496045

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35.

Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the beta 2-adrenoceptor.

Bond RA, Leff P, Johnson TD, Milano CA, Rockman HA, McMinn TR, Apparsundaram S, Hyek MF, Kenakin TP, Allen LF, et al.

Nature. 1995 Mar 16;374(6519):272-6.

PMID:
7885448

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36.

Definition of pharmacological receptors.

Kenakin TP, Bond RA, Bonner TI.

Pharmacol Rev. 1992 Sep;44(3):351-62. Review. No abstract available.

PMID:
1438521

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37.

Tissue response as a functional discriminator of receptor heterogeneity: effects of mixed receptor populations on Schild regressions.

Kenakin TP.

Mol Pharmacol. 1992 Apr;41(4):699-707.

PMID:
1569922

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38.

Biphasic dose-response curves to arecoline in rat atria-mediation by a single promiscuous receptor or two receptor subtypes?

Kenakin TP, Boselli C.

Naunyn Schmiedebergs Arch Pharmacol. 1991 Aug;344(2):201-5.

PMID:
1944613

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39.

The relative efficiency of beta adrenoceptor coupling to myocardial inotropy and diastolic relaxation: organ-selective treatment for diastolic dysfunction.

Kenakin TP, Ambrose JR, Irving PE.

J Pharmacol Exp Ther. 1991 Jun;257(3):1189-97.

PMID:
1675290

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40.

Promiscuous or heterogeneous muscarinic receptors in rat atria? II. Antagonism of responses to carbachol by pirenzepine.

Boselli C, Kenakin TP.

Eur J Pharmacol. 1990 Nov 20;191(1):49-57.

PMID:
2093000

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41.

Promiscuous or heterogeneous muscarinic receptors in rat atria? I. Schild analysis with simple competitive antagonists.

Kenakin TP, Boselli C.

Eur J Pharmacol. 1990 Nov 20;191(1):39-48.

PMID:
2092999

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42.

Theoretical effects of single and multiple transducer receptor coupling proteins on estimates of the relative potency of agonists.

Kenakin TP, Morgan PH.

Mol Pharmacol. 1989 Feb;35(2):214-22.

PMID:
2537459

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43.

Challenges for receptor theory as a tool for drug and drug receptor classification.

Kenakin TP.

Trends Pharmacol Sci. 1989 Jan;10(1):18-22. Review.

PMID:
2688212

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44.

KRAX is important operational determinant of tissue response. KRAX as parameter for classification.

Morgan PH, Lutz MW, Kenakin TP.

Trends Pharmacol Sci. 1988 Oct;9(10):351. No abstract available.

PMID:
3270957

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45.

Classification of phenoxybenzamine/prazosin-resistant contractions of rat spleen to norepinephrine by Schild analysis: similarities and differences to postsynaptic alpha-2 adrenoceptors.

Kenakin TP, Novak PJ.

J Pharmacol Exp Ther. 1988 Jan;244(1):206-12.

PMID:
2826768

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46.

A method to assess concomitant cardiac phosphodiesterase inhibition and positive inotropy.

Kenakin TP, Scott DL.

J Cardiovasc Pharmacol. 1987 Dec;10(6):658-66.

PMID:
2450236

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47.

Measurement of antagonist affinity for purine receptors of drugs producing concomitant phosphodiesterase blockade: the use of pharmacologic resultant analysis.

Kenakin TP, Beek D.

J Pharmacol Exp Ther. 1987 Nov;243(2):482-6.

PMID:
2445952

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48.

An in vitro analysis of purine-mediated renal vasoconstriction in rat isolated kidney.

Kenakin TP, Pike NB.

Br J Pharmacol. 1987 Feb;90(2):373-81.

PMID:
3828655
Free PMC Article

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49.

The effects on Schild regressions of antagonist removal from the receptor compartment by a saturable process.

Kenakin TP, Beek D.

Naunyn Schmiedebergs Arch Pharmacol. 1987 Feb;335(2):103-8.

PMID:
3561525

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50.

The quantification of relative efficacy of agonists.

Kenakin TP.

J Pharmacol Methods. 1985 Jul;13(4):281-308. Review.

PMID:
2991665

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