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Items: 1 to 50 of 162

1.

Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes.

Xu G, Gaul MD, Song F, Du F, Liang Y, DesJarlais RL, DiLoreto K, Shook B, Rentzeperis D, Santulli R, Eckardt A, Demarest K.

Bioorg Med Chem Lett. 2019 Oct 15;29(20):126668. doi: 10.1016/j.bmcl.2019.126668. Epub 2019 Sep 4.

PMID:
31519374
2.

Concerted 2-5A-Mediated mRNA Decay and Transcription Reprogram Protein Synthesis in the dsRNA Response.

Rath S, Prangley E, Donovan J, Demarest K, Wingreen NS, Meir Y, Korennykh A.

Mol Cell. 2019 Sep 19;75(6):1218-1228.e6. doi: 10.1016/j.molcel.2019.07.027. Epub 2019 Sep 4.

PMID:
31494033
3.

Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists.

Song F, Xu G, Gaul MD, Zhao B, Lu T, Zhang R, DesJarlais RL, DiLoreto K, Huebert N, Shook B, Rentzeperis D, Santulli R, Eckardt A, Demarest K.

Bioorg Med Chem Lett. 2019 Aug 1;29(15):1974-1980. doi: 10.1016/j.bmcl.2019.05.036. Epub 2019 May 18.

PMID:
31138472
4.

Real-time 2-5A kinetics suggest that interferons β and λ evade global arrest of translation by RNase L.

Chitrakar A, Rath S, Donovan J, Demarest K, Li Y, Sridhar RR, Weiss SR, Kotenko SV, Wingreen NS, Korennykh A.

Proc Natl Acad Sci U S A. 2019 Feb 5;116(6):2103-2111. doi: 10.1073/pnas.1818363116. Epub 2019 Jan 17.

5.

6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB1) Receptor Inverse Agonists and Chemical Modifications for Peripheral Selectivity.

Zhang YM, Greco MN, Macielag MJ, Teleha CA, DesJarlais RL, Tang Y, Ho G, Hou C, Chen C, Zhao S, Kauffman J, Camacho R, Qi J, Murray W, Demarest K, Leonard J.

J Med Chem. 2018 Nov 21;61(22):10276-10298. doi: 10.1021/acs.jmedchem.8b01467. Epub 2018 Oct 31.

PMID:
30339387
6.

Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.

Xu G, Gaul MD, Kuo GH, Du F, Xu JZ, Wallace N, Hinke S, Kirchner T, Silva J, Huebert ND, Lee S, Murray W, Liang Y, Demarest K.

Bioorg Med Chem Lett. 2018 Nov 15;28(21):3446-3453. doi: 10.1016/j.bmcl.2018.09.025. Epub 2018 Sep 19.

PMID:
30268701
7.

Potent Sodium/Glucose Cotransporter SGLT1/2 Dual Inhibition Improves Glycemic Control Without Marked Gastrointestinal Adaptation or Colonic Microbiota Changes in Rodents.

Du F, Hinke SA, Cavanaugh C, Polidori D, Wallace N, Kirchner T, Jennis M, Lang W, Kuo GH, Gaul MD, Lenhard J, Demarest K, Ajami NJ, Liang Y, Hornby PJ.

J Pharmacol Exp Ther. 2018 Jun;365(3):676-687. doi: 10.1124/jpet.118.248575. Epub 2018 Apr 19.

PMID:
29674332
8.

Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors.

Kuo GH, Gaul MD, Liang Y, Xu JZ, Du F, Hornby P, Xu G, Qi J, Wallace N, Lee S, Grant E, Murray WV, Demarest K.

Bioorg Med Chem Lett. 2018 Apr 15;28(7):1182-1187. doi: 10.1016/j.bmcl.2018.02.057. Epub 2018 Mar 1.

PMID:
29523385
9.

Discovery of Orally Efficacious Tetrahydrobenzimidazoles as TGR5 Agonists for Type 2 Diabetes.

Zhang X, Wall M, Sui Z, Kauffman J, Hou C, Chen C, Du F, Kirchner T, Liang Y, Johnson DL, Murray WV, Demarest K.

ACS Med Chem Lett. 2017 Apr 21;8(5):560-565. doi: 10.1021/acsmedchemlett.7b00116. eCollection 2017 May 11.

10.

Evaluation of anti-diabetic effect and gall bladder function with 2-thio-5-thiomethyl substituted imidazoles as TGR5 receptor agonists.

Zhang X, Sui Z, Kauffman J, Hou C, Chen C, Du F, Kirchner T, Liang Y, Johnson D, Murray WV, Demarest K.

Bioorg Med Chem Lett. 2017 Apr 15;27(8):1760-1764. doi: 10.1016/j.bmcl.2017.02.069. Epub 2017 Feb 28.

PMID:
28285911
11.

Canagliflozin: a sodium glucose co-transporter 2 inhibitor for the treatment of type 2 diabetes mellitus.

Rosenthal N, Meininger G, Ways K, Polidori D, Desai M, Qiu R, Alba M, Vercruysse F, Balis D, Shaw W, Edwards R, Bull S, Di Prospero N, Sha S, Rothenberg P, Canovatchel W, Demarest K.

Ann N Y Acad Sci. 2015 Nov;1358:28-43. doi: 10.1111/nyas.12852. Epub 2015 Aug 25. Review.

PMID:
26305874
12.

Pharmacodynamic effects of canagliflozin, a sodium glucose co-transporter 2 inhibitor, from a randomized study in patients with type 2 diabetes.

Sha S, Devineni D, Ghosh A, Polidori D, Hompesch M, Arnolds S, Morrow L, Spitzer H, Demarest K, Rothenberg P.

PLoS One. 2014 Sep 30;9(9):e110069. doi: 10.1371/journal.pone.0110069. eCollection 2014.

13.

Aspen shaving versus chip bedding: effects on breeding and behavior.

Jackson E, Demarest K, Eckert WJ, Cates-Gatto C, Nadav T, Cates LN, Howard H, Roberts AJ.

Lab Anim. 2015 Jan;49(1):46-56. doi: 10.1177/0023677214553320. Epub 2014 Sep 26.

PMID:
25260358
14.

Pharmacodynamic effects of canagliflozin, a sodium glucose co-transporter 2 inhibitor, from a randomized study in patients with type 2 diabetes.

Sha S, Devineni D, Ghosh A, Polidori D, Hompesch M, Arnolds S, Morrow L, Spitzer H, Demarest K, Rothenberg P.

PLoS One. 2014 Aug 28;9(8):e105638. doi: 10.1371/journal.pone.0105638. eCollection 2014.

15.

4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: part 2. Pyridazine-based analogs.

Yang SM, Tang Y, Rano T, Lu H, Kuo GH, Gaul MD, Li Y, Ho G, Lang W, Conway JG, Liang Y, Lenhard JM, Demarest KT, Murray WV.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1437-41. doi: 10.1016/j.bmcl.2013.12.075. Epub 2013 Dec 27.

PMID:
24405703
16.

4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: urea-based analogs.

Yang SM, Tang Y, Zhang R, Lu H, Kuo GH, Gaul MD, Li Y, Ho G, Conway JG, Liang Y, Lenhard JM, Demarest KT, Murray WV.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6773-6. doi: 10.1016/j.bmcl.2013.09.096. Epub 2013 Oct 9.

PMID:
24153205
17.

Beneficial metabolic effects of CB1R anti-sense oligonucleotide treatment in diet-induced obese AKR/J mice.

Tang Y, Ho G, Li Y, Hall MA, Hills RL, Black SC, Liang Y, Demarest KT.

PLoS One. 2012;7(8):e42134. doi: 10.1371/journal.pone.0042134. Epub 2012 Aug 3.

18.

Phase 0 study of the inhibition of cholesteryl ester transfer protein activity by JNJ-28545595 in plasma from normolipidemic and dyslipidemic humans.

Sarich TC, Connelly MA, Schranz DB, Ghosh A, Manitpisitkul P, Leary ET, Rothenberg P, Demarest KT, Damiano BP.

Int J Clin Pharmacol Ther. 2012 Aug;50(8):584-94. doi: 10.5414/CP201627.

PMID:
22578199
19.

The use of stable isotope-labeled glycerol and oleic acid to differentiate the hepatic functions of DGAT1 and -2.

Qi J, Lang W, Geisler JG, Wang P, Petrounia I, Mai S, Smith C, Askari H, Struble GT, Williams R, Bhanot S, Monia BP, Bayoumy S, Grant E, Caldwell GW, Todd MJ, Liang Y, Gaul MD, Demarest KT, Connelly MA.

J Lipid Res. 2012 Jun;53(6):1106-16. doi: 10.1194/jlr.M020156. Epub 2012 Apr 3.

20.

Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models.

Liang Y, Arakawa K, Ueta K, Matsushita Y, Kuriyama C, Martin T, Du F, Liu Y, Xu J, Conway B, Conway J, Polidori D, Ways K, Demarest K.

PLoS One. 2012;7(2):e30555. doi: 10.1371/journal.pone.0030555. Epub 2012 Feb 15.

21.

Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile.

Semple G, Lehmann J, Wong A, Ren A, Bruce M, Shin YJ, Sage CR, Morgan M, Chen WC, Sebring K, Chu ZL, Leonard JN, Al-Shamma H, Grottick AJ, Du F, Liang Y, Demarest K, Jones RM.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-5. doi: 10.1016/j.bmcl.2011.12.092. Epub 2011 Dec 30.

PMID:
22264481
22.

Canagliflozin, a novel inhibitor of sodium glucose co-transporter 2, dose dependently reduces calculated renal threshold for glucose excretion and increases urinary glucose excretion in healthy subjects.

Sha S, Devineni D, Ghosh A, Polidori D, Chien S, Wexler D, Shalayda K, Demarest K, Rothenberg P.

Diabetes Obes Metab. 2011 Jul;13(7):669-72. doi: 10.1111/j.1463-1326.2011.01406.x.

PMID:
21457428
23.

Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.

Semple G, Ren A, Fioravanti B, Pereira G, Calderon I, Choi K, Xiong Y, Shin YJ, Gharbaoui T, Sage CR, Morgan M, Xing C, Chu ZL, Leonard JN, Grottick AJ, Al-Shamma H, Liang Y, Demarest KT, Jones RM.

Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41. doi: 10.1016/j.bmcl.2011.03.007. Epub 2011 Mar 13.

PMID:
21444206
24.

In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease.

Shook BC, Rassnick S, Osborne MC, Davis S, Westover L, Boulet J, Hall D, Rupert KC, Heintzelman GR, Hansen K, Chakravarty D, Bullington JL, Russell R, Branum S, Wells KM, Damon S, Youells S, Li X, Beauchamp DA, Palmer D, Reyes M, Demarest K, Tang Y, Rhodes K, Jackson PF.

J Med Chem. 2010 Nov 25;53(22):8104-15. doi: 10.1021/jm100971t. Epub 2010 Oct 25.

PMID:
20973483
25.

Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

Shook BC, Rassnick S, Hall D, Rupert KC, Heintzelman GR, Hansen K, Chakravarty D, Bullington JL, Scannevin RH, Magliaro B, Westover L, Carroll K, Lampron L, Russell R, Branum S, Wells K, Damon S, Youells S, Li X, Osbourne M, Demarest K, Tang Y, Rhodes K, Jackson PF.

Bioorg Med Chem Lett. 2010 May 1;20(9):2864-7. doi: 10.1016/j.bmcl.2010.03.042. Epub 2010 Mar 11.

PMID:
20347304
26.

Synthesis and discovery of 2,3-dihydro-3,8-diphenylbenzo[1,4]oxazines as a novel class of potent cholesteryl ester transfer protein inhibitors.

Wang A, Prouty CP, Pelton PD, Yong M, Demarest KT, Murray WV, Kuo GH.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1432-5. doi: 10.1016/j.bmcl.2009.12.096. Epub 2010 Jan 4.

PMID:
20089400
27.

Torcetrapib produces endothelial dysfunction independent of cholesteryl ester transfer protein inhibition.

Connelly MA, Parry TJ, Giardino EC, Huang Z, Cheung WM, Chen C, Cools F, Van der Linde H, Gallacher DJ, Kuo GH, Sarich TC, Demarest KT, Damiano BP.

J Cardiovasc Pharmacol. 2010 May;55(5):459-68. doi: 10.1097/FJC.0b013e3181cf03cb.

PMID:
20051879
28.

Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform.

Rano TA, Sieber-McMaster E, Pelton PD, Yang M, Demarest KT, Kuo GH.

Bioorg Med Chem Lett. 2009 May 1;19(9):2456-60. doi: 10.1016/j.bmcl.2009.03.051. Epub 2009 Mar 18.

PMID:
19339179
30.

Synthesis and SAR study of novel pseudo-steroids as potent and selective progesterone receptor antagonists.

Jain N, Allan G, Linton O, Tannenbaum P, Chen X, Xu J, Zhu P, Gunnet J, Demarest K, Lundeen S, Murray W, Sui Z.

Bioorg Med Chem Lett. 2009 Jul 15;19(14):3977-80. doi: 10.1016/j.bmcl.2009.01.095. Epub 2009 Jan 31.

PMID:
19217285
31.

Discovery and SAR of para-alkylthiophenoxyacetic acids as potent and selective PPARdelta agonists.

Zhang R, Deangelis A, Wang A, Sieber-McMaster E, Li X, Russell R, Pelton P, Xu J, Zhu P, Zhou L, Demarest K, Murray WV, Kuo GH.

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1101-4. doi: 10.1016/j.bmcl.2008.12.113. Epub 2009 Jan 8.

PMID:
19168353
32.

Improvement of dyslipidemia, insulin sensitivity, and energy balance by a peroxisome proliferator-activated receptor alpha agonist.

Chen X, Matthews J, Zhou L, Pelton P, Liang Y, Xu J, Yang M, Cryan E, Rybczynski P, Demarest K.

Metabolism. 2008 Nov;57(11):1516-25. doi: 10.1016/j.metabol.2008.06.005.

PMID:
18940388
33.

Pharmacological characterization of RWJ-676070, a dual vasopressin V(1A)/V(2) receptor antagonist.

Gunnet JW, Wines P, Xiang M, Rybczynski P, Andrade-Gordon P, de Garavilla L, Parry TJ, Cheung WM, Minor L, Demarest KT, Maryanoff BE, Damiano BP.

Eur J Pharmacol. 2008 Aug 20;590(1-3):333-42. doi: 10.1016/j.ejphar.2008.06.010. Epub 2008 Jun 7.

PMID:
18599033
34.

Synthesis and structure-activity relationships of thiadiazole-derivatives as potent and orally active peroxisome proliferator-activated receptors alpha/delta dual agonists.

Shen L, Zhang Y, Wang A, Sieber-McMaster E, Chen X, Pelton P, Xu JZ, Yang M, Zhu P, Zhou L, Reuman M, Hu Z, Russell R, Gibbs AC, Ross H, Demarest K, Murray WV, Kuo GH.

Bioorg Med Chem. 2008 Mar 15;16(6):3321-41. Epub 2007 Dec 8.

PMID:
18155554
35.

Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.

Matthews JM, Chen X, Cryan E, Hlasta DJ, Rybczynski PJ, Strauss K, Tang Y, Xu JZ, Yang M, Zhou L, Demarest KT.

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6773-8. Epub 2007 Oct 17.

PMID:
18029176
36.

Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.

Xiang MA, Rybczynski PJ, Patel M, Chen RH, McComsey DF, Zhang HC, Gunnet JW, Look R, Wang Y, Minor LK, Zhong HM, Villani FJ, Demarest KT, Damiano BP, Maryanoff BE.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6623-8. Epub 2007 Sep 19.

PMID:
17942308
37.

Synthesis and identification of [1,2,4]thiadiazole derivatives as a new series of potent and orally active dual agonists of peroxisome proliferator-activated receptors alpha and delta.

Shen L, Zhang Y, Wang A, Sieber-McMaster E, Chen X, Pelton P, Xu JZ, Yang M, Zhu P, Zhou L, Reuman M, Hu Z, Russell R, Gibbs AC, Ross H, Demarest K, Murray WV, Kuo GH.

J Med Chem. 2007 Aug 9;50(16):3954-63. Epub 2007 Jul 4.

PMID:
17608467
38.

Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists.

Zhang R, Wang A, DeAngelis A, Pelton P, Xu J, Zhu P, Zhou L, Demarest K, Murray WV, Kuo GH.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3855-9. Epub 2007 May 10.

PMID:
17524639
39.

Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists.

Song F, Lu S, Gunnet J, Xu JZ, Wines P, Proost J, Liang Y, Baumann C, Lenhard J, Murray WV, Demarest KT, Kuo GH.

J Med Chem. 2007 Jun 14;50(12):2807-17. Epub 2007 May 15.

PMID:
17500511
40.

Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists.

Kang FA, Guan J, Jain N, Allan G, Linton O, Tannenbaum P, Chen X, Xu J, Zhu P, Gunnet J, Demarest K, Lundeen S, Sui Z.

Bioorg Med Chem Lett. 2007 May 1;17(9):2531-4. Epub 2007 Feb 8.

PMID:
17317167
41.

A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release.

Chu ZL, Jones RM, He H, Carroll C, Gutierrez V, Lucman A, Moloney M, Gao H, Mondala H, Bagnol D, Unett D, Liang Y, Demarest K, Semple G, Behan DP, Leonard J.

Endocrinology. 2007 Jun;148(6):2601-9. Epub 2007 Feb 8. Erratum in: Endocrinology. 2007 Oct;148(10):4753.

PMID:
17289847
42.

Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.

Jiang W, Fiordeliso JJ, Allan G, Linton O, Tannenbaum P, Xu J, Zhu P, Gunnet J, Demarest K, Lundeen S, Sui Z.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1471-4. Epub 2006 Oct 5.

PMID:
17258455
43.

Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.

Kang FA, Allan G, Guan J, Jain N, Linton O, Tannenbaum P, Xu J, Zhu P, Gunnet J, Chen X, Demarest K, Lundeen S, Sui Z.

Bioorg Med Chem Lett. 2007 Feb 15;17(4):907-10. Epub 2006 Dec 1.

PMID:
17169557
44.

Human epidermoid A431 cells express functional nicotinic acid receptor HM74a.

Zhou L, Tang Y, Cryan EV, Demarest KT.

Mol Cell Biochem. 2007 Jan;294(1-2):243-8. Epub 2006 Nov 24.

PMID:
17124637
46.

Novel phosphorus-containing 17beta-side chain mifepristone analogues as progesterone receptor antagonists.

Jiang W, Allan G, Chen X, Fiordeliso JJ, Linton O, Tannenbaum P, Xu J, Zhu P, Gunnet J, Demarest K, Lundeen S, Sui Z.

Steroids. 2006 Nov;71(11-12):949-54. Epub 2006 Aug 28.

PMID:
16934845
47.

New progesterone receptor antagonists: phosphorus-containing 11beta-aryl-substituted steroids.

Jiang W, Allan G, Fiordeliso JJ, Linton O, Tannenbaum P, Xu J, Zhu P, Gunnet J, Demarest K, Lundeen S, Sui Z.

Bioorg Med Chem. 2006 Oct 1;14(19):6726-32. Epub 2006 Jun 27.

PMID:
16806946
48.

Enhancement of arachidonic acid signaling pathway by nicotinic acid receptor HM74A.

Tang Y, Zhou L, Gunnet JW, Wines PG, Cryan EV, Demarest KT.

Biochem Biophys Res Commun. 2006 Jun 23;345(1):29-37. Epub 2006 Apr 25.

PMID:
16674924
49.

Synthesis and SAR of 1,3-disubstituted cyclohexylmethyl urea and amide derivatives as non-peptidic motilin receptor antagonists.

Johnson SG, Gunnet JW, Moore JB, Miller W, Wines P, Rivero RA, Combs D, Demarest KT.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3362-6. Epub 2006 May 2.

PMID:
16650762
50.

Characterization of RWJ-351647, a novel nonpeptide vasopressin V2 receptor antagonist.

Gunnet JW, Matthews JM, Maryanoff BE, de Garavilla L, Andrade-Gordon P, Damiano B, Hageman W, Look R, Stahle P, Streeter AJ, Wines PG, Demarest KT.

Clin Exp Pharmacol Physiol. 2006 Apr;33(4):320-6.

PMID:
16620295

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