Gentles RG - Search Results

1

In vitro Characterization of a small molecule inhibitor of the alanine serine cysteine transporter -1 (SLC7A10).

Brown JM, Hunihan L, Prack MM, Harden DG, Bronson J, Dzierba CD, Gentles RG, Hendricson A, Krause R, Macor JE, Westphal RS. Brown JM, et al. Among authors: gentles rg. J Neurochem. 2014 Apr;129(2):275-83. doi: 10.1111/jnc.12618. Epub 2013 Dec 10. J Neurochem. 2014. PMID: 24266811 Free article.

2

Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.

Gentles RG, Grant-Young K, Hu S, Huang Y, Poss MA, Andres C, Fiedler T, Knox R, Lodge N, Weaver CD, Harden DG. Gentles RG, et al. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5316-9. doi: 10.1016/j.bmcl.2008.08.023. Epub 2008 Aug 14. Bioorg Med Chem Lett. 2008. PMID: 18774291

3

Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine K(Ca) channel blockers.

Gentles RG, Hu S, Huang Y, Grant-Young K, Poss MA, Andres C, Fiedler T, Knox R, Lodge N, Weaver CD, Harden DG. Gentles RG, et al. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5694-7. doi: 10.1016/j.bmcl.2008.08.026. Epub 2008 Aug 14. Bioorg Med Chem Lett. 2008. PMID: 18824351

4

Screening and characterization of reactive compounds with in vitro peptide-trapping and liquid chromatography/high-resolution accurate mass spectrometry.

Wei C, Chupak LS, Philip T, Johnson BM, Gentles R, Drexler DM. Wei C, et al. J Biomol Screen. 2014 Feb;19(2):297-307. doi: 10.1177/1087057113492852. Epub 2013 Jun 24. J Biomol Screen. 2014. PMID: 23796688

5

Identification of small molecules that selectively inhibit diacylglycerol lipase-α activity.

Appiah KK, Blat Y, Robertson BJ, Pearce BC, Pedicord DL, Gentles RG, Yu XC, Mseeh F, Nguyen N, Swaffield JC, Harden DG, Westphal RS, Banks MN, O'Connell JC. Appiah KK, et al. Among authors: gentles rg. J Biomol Screen. 2014 Apr;19(4):595-605. doi: 10.1177/1087057113511111. Epub 2013 Nov 15. J Biomol Screen. 2014. PMID: 24241710

6

Discovery of D1 Dopamine Receptor Positive Allosteric Modulators: Characterization of Pharmacology and Identification of Residues that Regulate Species Selectivity.

Lewis MA, Hunihan L, Watson J, Gentles RG, Hu S, Huang Y, Bronson J, Macor JE, Beno BR, Ferrante M, Hendricson A, Knox RJ, Molski TF, Kong Y, Cvijic ME, Rockwell KL, Weed MR, Cacace AM, Westphal RS, Alt A, Brown JM. Lewis MA, et al. Among authors: gentles rg. J Pharmacol Exp Ther. 2015 Sep;354(3):340-9. doi: 10.1124/jpet.115.224071. Epub 2015 Jun 24. J Pharmacol Exp Ther. 2015. PMID: 26109678

7

Evidence for Classical Cholinergic Toxicity Associated with Selective Activation of M1 Muscarinic Receptors.

Alt A, Pendri A, Bertekap RL Jr, Li G, Benitex Y, Nophsker M, Rockwell KL, Burford NT, Sum CS, Chen J, Herbst JJ, Ferrante M, Hendricson A, Cvijic ME, Westphal RS, O'Connell J, Banks M, Zhang L, Gentles RG, Jenkins S, Loy J, Macor JE. Alt A, et al. Among authors: gentles rg. J Pharmacol Exp Ther. 2016 Feb;356(2):293-304. doi: 10.1124/jpet.115.226910. Epub 2015 Nov 18. J Pharmacol Exp Ther. 2016. PMID: 26582730

8

Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.

Chupak LS, Zheng X, Hu S, Huang Y, Ding M, Lewis MA, Westphal RS, Blat Y, McClure A, Gentles RG. Chupak LS, et al. Among authors: gentles rg. Bioorg Med Chem. 2016 Apr 1;24(7):1455-68. doi: 10.1016/j.bmc.2016.02.006. Epub 2016 Feb 16. Bioorg Med Chem. 2016. PMID: 26917221

9

A Small Molecule Inhibitor Selectively Induces Apoptosis in Cells Transformed by High Risk Human Papilloma Viruses.

Sheaffer AK, Lee MS, Qi H, Chaniewski S, Zheng X, Farr GA, Esposito K, Harden D, Lei M, Schweizer L, Friborg J, Agler M, McPhee F, Gentles R, Beno BR, Chupak L, Mason S. Sheaffer AK, et al. PLoS One. 2016 Jun 9;11(6):e0155909. doi: 10.1371/journal.pone.0155909. eCollection 2016. PLoS One. 2016. PMID: 27280728 Free PMC article.

10

Triazolopyridine ethers as potent, orally active mGlu₂ positive allosteric modulators for treating schizophrenia.

Higgins MA, Marcin LR, Christopher Zusi F, Gentles R, Ding M, Pearce BC, Easton A, Kostich WA, Seager MA, Bourin C, Bristow LJ, Johnson KA, Miller R, Hogan J, Whiterock V, Gulianello M, Ferrante M, Huang Y, Hendricson A, Alt A, Macor JE, Bronson JJ. Higgins MA, et al. Bioorg Med Chem. 2017 Jan 15;25(2):496-513. doi: 10.1016/j.bmc.2016.11.018. Epub 2016 Nov 14. Bioorg Med Chem. 2017. PMID: 27914948

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