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Items: 13

1.

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.

PMID:
29426768
2.

Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties.

Brust TF, Alongkronrusmee D, Soto-Velasquez M, Baldwin TA, Ye Z, Dai M, Dessauer CW, van Rijn RM, Watts VJ.

Sci Signal. 2017 Feb 21;10(467). pii: eaah5381. doi: 10.1126/scisignal.aah5381.

3.

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.

4.

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.

5.

Bisamidate Prodrugs of 2-Substituted 9-[2-(Phosphonomethoxy)ethyl]adenine (PMEA, adefovir) as Selective Inhibitors of Adenylate Cyclase Toxin from Bordetella pertussis.

Česnek M, Jansa P, Šmídková M, Mertlíková-Kaiserová H, Dračínský M, Brust TF, Pávek P, Trejtnar F, Watts VJ, Janeba Z.

ChemMedChem. 2015 Aug;10(8):1351-64. doi: 10.1002/cmdc.201500183. Epub 2015 Jul 1.

PMID:
26136378
6.

Gα(i/o)-coupled receptor-mediated sensitization of adenylyl cyclase: 40 years later.

Brust TF, Conley JM, Watts VJ.

Eur J Pharmacol. 2015 Sep 15;763(Pt B):223-32. doi: 10.1016/j.ejphar.2015.05.014. Epub 2015 May 14. Review.

7.

Palladium-catalyzed regio- and stereoselective γ-arylation of tertiary allylic amines: identification of potent adenylyl cyclase inhibitors.

Ye Z, Brust TF, Watts VJ, Dai M.

Org Lett. 2015 Feb 20;17(4):892-5. doi: 10.1021/ol503748t. Epub 2015 Feb 10.

8.

Bias analyses of preclinical and clinical D2 dopamine ligands: studies with immediate and complex signaling pathways.

Brust TF, Hayes MP, Roman DL, Burris KD, Watts VJ.

J Pharmacol Exp Ther. 2015 Mar;352(3):480-93. doi: 10.1124/jpet.114.220293. Epub 2014 Dec 24.

9.

New functional activity of aripiprazole revealed: Robust antagonism of D2 dopamine receptor-stimulated Gβγ signaling.

Brust TF, Hayes MP, Roman DL, Watts VJ.

Biochem Pharmacol. 2015 Jan 1;93(1):85-91. doi: 10.1016/j.bcp.2014.10.014. Epub 2014 Nov 7.

10.

Polydopamine-based simple and versatile surface modification of polymeric nano drug carriers.

Park J, Brust TF, Lee HJ, Lee SC, Watts VJ, Yeo Y.

ACS Nano. 2014 Apr 22;8(4):3347-56. doi: 10.1021/nn405809c. Epub 2014 Mar 19.

11.

Drug-induced sensitization of adenylyl cyclase: assay streamlining and miniaturization for small molecule and siRNA screening applications.

Conley JM, Brust TF, Xu R, Burris KD, Watts VJ.

J Vis Exp. 2014 Jan 27;(83):e51218. doi: 10.3791/51218.

12.

Discovery of antagonists of tick dopamine receptors via chemical library screening and comparative pharmacological analyses.

Ejendal KF, Meyer JM, Brust TF, Avramova LV, Hill CA, Watts VJ.

Insect Biochem Mol Biol. 2012 Nov;42(11):846-53.

PMID:
23213654
13.

A "genome-to-lead" approach for insecticide discovery: pharmacological characterization and screening of Aedes aegypti D(1)-like dopamine receptors.

Meyer JM, Ejendal KF, Avramova LV, Garland-Kuntz EE, Giraldo-Calderón GI, Brust TF, Watts VJ, Hill CA.

PLoS Negl Trop Dis. 2012 Jan;6(1):e1478. doi: 10.1371/journal.pntd.0001478. Epub 2012 Jan 24.

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