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Items: 1 to 20 of 182

1.

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
2.

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.

3.

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.

PMID:
27389877
4.

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
5.

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.

PMID:
26991104
6.

Theoretical Aspects of GPCR-Ligand Complex Pharmacology.

Kenakin T.

Chem Rev. 2016 Feb 9. [Epub ahead of print]

PMID:
26856272
7.

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

Kenakin TP.

Pharmacol Res. 2016 Jan 21. pii: S1043-6618(16)00024-4. doi: 10.1016/j.phrs.2016.01.022. [Epub ahead of print]

PMID:
26804250
8.

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.

9.

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.

PMID:
26550826
10.

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.

PMID:
26506455
11.

New Lives for Seven Transmembrane Receptors as Drug Targets.

Kenakin T.

Trends Pharmacol Sci. 2015 Nov;36(11):705-6. doi: 10.1016/j.tips.2015.09.004. Epub 2015 Oct 16. No abstract available.

PMID:
26482172
12.

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
13.

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
14.

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.

15.

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.

16.

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):2195-203. doi: 10.1016/j.bmc.2015.02.058. Epub 2015 Mar 7.

17.

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
18.

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.

19.

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.

20.

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
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