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Items: 1 to 50 of 201

1.

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. 2018 Sep 20. doi: 10.1021/acschemneuro.8b00396. [Epub ahead of print]

PMID:
30188693
2.

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
3.

Equilibrium Assays Are Required to Accurately Characterize the Activity Profiles of Drugs Modulating Gq-Protein-Coupled Receptors.

Bdioui S, Verdi J, Pierre N, Trinquet E, Roux T, Kenakin T.

Mol Pharmacol. 2018 Sep;94(3):992-1006. doi: 10.1124/mol.118.112573. Epub 2018 Jun 28.

PMID:
29954837
4.

PAM-Antagonists: A Better Way to Block Pathological Receptor Signaling?

Kenakin T, Strachan RT.

Trends Pharmacol Sci. 2018 Aug;39(8):748-765. doi: 10.1016/j.tips.2018.05.001. Epub 2018 Jun 7. Review.

PMID:
29885909
5.

Is the Quest for Signaling Bias Worth the Effort?

Kenakin T.

Mol Pharmacol. 2018 Apr;93(4):266-269. doi: 10.1124/mol.117.111187. Epub 2018 Jan 18.

PMID:
29348268
6.

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
7.

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
8.

A Scale of Agonism and Allosteric Modulation for Assessment of Selectivity, Bias, and Receptor Mutation.

Kenakin T.

Mol Pharmacol. 2017 Oct;92(4):414-424. doi: 10.1124/mol.117.108787. Epub 2017 Jul 5. Review. Erratum in: Mol Pharmacol. 2017 Nov;92 (5):501.

PMID:
28679508
9.

Design and Synthesis of γ- and δ-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity.

Davoren JE, Garnsey M, Pettersen B, Brodney MA, Edgerton JR, Fortin JP, Grimwood S, Harris AR, Jenkinson S, Kenakin T, Lazzaro JT, Lee CW, Lotarski SM, Nottebaum L, O'Neil SV, Popiolek M, Ramsey S, Steyn SJ, Thorn CA, Zhang L, Webb D.

J Med Chem. 2017 Aug 10;60(15):6649-6663. doi: 10.1021/acs.jmedchem.7b00597. Epub 2017 Jul 26.

PMID:
28598634
10.

Chemical genomic analysis of GPR35 signaling.

Hu HH, Deng H, Ling S, Sun H, Kenakin T, Liang X, Fang Y.

Integr Biol (Camb). 2017 May 22;9(5):451-463. doi: 10.1039/c7ib00005g.

PMID:
28425521
11.

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
12.

The Quantitative Characterization of Functional Allosteric Effects.

Kenakin T.

Curr Protoc Pharmacol. 2017 Mar 17;76:9.22.1-9.22.10. doi: 10.1002/cpph.18.

PMID:
28306151
13.

Signaling bias in drug discovery.

Kenakin T.

Expert Opin Drug Discov. 2017 Apr;12(4):321-333. doi: 10.1080/17460441.2017.1297417. Epub 2017 Mar 9. Review.

PMID:
28277840
14.

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.

15.

A New Molecular Mechanism To Engineer Protean Agonism at a G Protein-Coupled Receptor.

De Min A, Matera C, Bock A, Holze J, Kloeckner J, Muth M, Traenkle C, De Amici M, Kenakin T, Holzgrabe U, Dallanoce C, Kostenis E, Mohr K, Schrage R.

Mol Pharmacol. 2017 Apr;91(4):348-356. doi: 10.1124/mol.116.107276. Epub 2017 Feb 6.

PMID:
28167741
16.

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
17.

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.

18.

New Modalities in Drug Therapy: Modifying Ongoing Chemical Conversations in the Brain.

Kenakin T.

ACS Chem Neurosci. 2016 Nov 16;7(11):1472-1473. Epub 2016 Oct 14.

PMID:
27739675
19.

Design and Discovery of Functionally Selective Serotonin 2C (5-HT2C) Receptor Agonists.

Cheng J, McCorvy JD, Giguere PM, Zhu H, Kenakin T, Roth BL, Kozikowski AP.

J Med Chem. 2016 Nov 10;59(21):9866-9880. Epub 2016 Oct 25.

PMID:
27726356
20.

Measurement of Receptor Signaling Bias.

Kenakin T.

Curr Protoc Pharmacol. 2016 Sep 16;74:2.15.1-2.15.15. doi: 10.1002/cpph.11.

PMID:
27636109
21.

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.

22.

Receptor antagonism/agonism can be uncoupled from pharmacoperone activity.

Janovick JA, Spicer TP, Smith E, Bannister TD, Kenakin T, Scampavia L, Conn PM.

Mol Cell Endocrinol. 2016 Oct 15;434:176-85. doi: 10.1016/j.mce.2016.07.003. Epub 2016 Jul 4.

23.

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
24.

A Molecular Mechanism for Sequential Activation of a G Protein-Coupled Receptor.

Grundmann M, Tikhonova IG, Hudson BD, Smith NJ, Mohr K, Ulven T, Milligan G, Kenakin T, Kostenis E.

Cell Chem Biol. 2016 Mar 17;23(3):392-403. doi: 10.1016/j.chembiol.2016.02.014.

25.

Theoretical Aspects of GPCR-Ligand Complex Pharmacology.

Kenakin T.

Chem Rev. 2017 Jan 11;117(1):4-20. doi: 10.1021/acs.chemrev.5b00561. Epub 2016 Feb 9. Review.

PMID:
26856272
26.

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
27.

Editorial: Orphan GPCRs As Emerging Drug Targets.

Fang Y, Kenakin T, Liu C.

Front Pharmacol. 2015 Dec 15;6:295. doi: 10.3389/fphar.2015.00295. eCollection 2015. No abstract available.

28.

Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65.

Huang XP, Karpiak J, Kroeze WK, Zhu H, Chen X, Moy SS, Saddoris KA, Nikolova VD, Farrell MS, Wang S, Mangano TJ, Deshpande DA, Jiang A, Penn RB, Jin J, Koller BH, Kenakin T, Shoichet BK, Roth BL.

Nature. 2015 Nov 26;527(7579):477-83. doi: 10.1038/nature15699. Epub 2015 Nov 9.

29.

The mass action equation in pharmacology.

Kenakin T.

Br J Clin Pharmacol. 2016 Jan;81(1):41-51. doi: 10.1111/bcp.12810. Epub 2015 Dec 21. Review.

30.

New Lives for Seven Transmembrane Receptors as Drug Targets.

Kenakin T.

Trends Pharmacol Sci. 2015 Nov;36(11):705-706. doi: 10.1016/j.tips.2015.09.004. Epub 2015 Oct 16. No abstract available.

PMID:
26482172
31.

The Measurement of Receptor Signaling Bias.

Kenakin T.

Methods Mol Biol. 2015;1335:163-76. doi: 10.1007/978-1-4939-2914-6_11.

PMID:
26260600
32.

The Effective Application of Biased Signaling to New Drug Discovery.

Kenakin T.

Mol Pharmacol. 2015 Dec;88(6):1055-61. doi: 10.1124/mol.115.099770. Epub 2015 Jul 2. Review.

PMID:
26138073
33.

N-linked glycosylation of protease-activated receptor-1 at extracellular loop 2 regulates G-protein signaling bias.

Soto AG, Smith TH, Chen B, Bhattacharya S, Cordova IC, Kenakin T, Vaidehi N, Trejo J.

Proc Natl Acad Sci U S A. 2015 Jul 7;112(27):E3600-8. doi: 10.1073/pnas.1508838112. Epub 2015 Jun 22.

34.

Gaddum Memorial Lecture 2014: receptors as an evolving concept: from switches to biased microprocessors.

Kenakin T.

Br J Pharmacol. 2015 Sep;172(17):4238-53. doi: 10.1111/bph.13217. Epub 2015 Jul 21. Review. Erratum in: Br J Pharmacol. 2016 Jan;173(2):412.

35.

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.

36.

What is pharmacological 'affinity'? Relevance to biased agonism and antagonism.

Kenakin T.

Trends Pharmacol Sci. 2014 Sep;35(9):434-41. doi: 10.1016/j.tips.2014.06.003. Epub 2014 Jul 17.

PMID:
25042457
37.

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
38.

The tail wags the dog: possible mechanism for reverse allosteric control of ligand-activated channels.

Vardy E, Kenakin T.

Br J Pharmacol. 2014 Apr;171(7):1614-6. doi: 10.1111/bph.12550.

39.

Quantifying biased β-arrestin signaling.

Kenakin T.

Handb Exp Pharmacol. 2014;219:57-83. doi: 10.1007/978-3-642-41199-1_3.

PMID:
24292824
40.

Replicated, replicable and relevant-target engagement and pharmacological experimentation in the 21st century.

Kenakin T, Bylund DB, Toews ML, Mullane K, Winquist RJ, Williams M.

Biochem Pharmacol. 2014 Jan 1;87(1):64-77. doi: 10.1016/j.bcp.2013.10.024. Epub 2013 Nov 19. Review.

PMID:
24269285
41.

Role of the N-terminal region in G protein-coupled receptor functions: negative modulation revealed by 5-HT2B receptor polymorphisms.

Belmer A, Doly S, Setola V, Banas SM, Moutkine I, Boutourlinsky K, Kenakin T, Maroteaux L.

Mol Pharmacol. 2014 Jan;85(1):127-38. doi: 10.1124/mol.113.089086. Epub 2013 Oct 30.

42.

Identification of novel functionally selective κ-opioid receptor scaffolds.

White KL, Scopton AP, Rives ML, Bikbulatov RV, Polepally PR, Brown PJ, Kenakin T, Javitch JA, Zjawiony JK, Roth BL.

Mol Pharmacol. 2014 Jan;85(1):83-90. doi: 10.1124/mol.113.089649. Epub 2013 Oct 10.

43.

Analytical pharmacology and allosterism: the importance of quantifying drug parameters in drug discovery.

Kenakin T.

Drug Discov Today Technol. 2013 Summer;10(2):e229-35. doi: 10.1016/j.ddtec.2012.07.006. Review.

PMID:
24050273
44.

Defining and characterizing drug/compound function.

Kenakin T, Williams M.

Biochem Pharmacol. 2014 Jan 1;87(1):40-63. doi: 10.1016/j.bcp.2013.07.033. Epub 2013 Aug 15. Review.

PMID:
23954707
45.

Measurements of ligand bias and functional affinity.

Kenakin T, Christopoulos A.

Nat Rev Drug Discov. 2013 Jun;12(6):483. doi: 10.1038/nrd3954-c2. Epub 2013 May 17. No abstract available.

PMID:
23681003
46.

Allosteric drug. Preface.

Kenakin T.

Prog Mol Biol Transl Sci. 2013;115:xi-xiii. doi: 10.1016/B978-0-12-394587-7.10000-4. No abstract available.

PMID:
23415101
47.

Signalling bias in new drug discovery: detection, quantification and therapeutic impact.

Kenakin T, Christopoulos A.

Nat Rev Drug Discov. 2013 Mar;12(3):205-16. doi: 10.1038/nrd3954. Epub 2012 Feb 15. Review.

PMID:
23411724
48.

Allosteric drugs and seven transmembrane receptors.

Kenakin T.

Curr Top Med Chem. 2013;13(1):5-13.

PMID:
23409762
49.

Making receptors a reality: the 2012 Nobel Prize in Chemistry.

Kenakin T.

Trends Pharmacol Sci. 2013 Jan;34(1):2-5. doi: 10.1016/j.tips.2012.11.003. Epub 2012 Dec 13. No abstract available.

PMID:
23246456
50.

New concepts in pharmacological efficacy at 7TM receptors: IUPHAR review 2.

Kenakin T.

Br J Pharmacol. 2013 Feb;168(3):554-75. doi: 10.1111/j.1476-5381.2012.02223.x. Review.

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