PubMed

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. Epub 2009 Mar 18.PMID: 19339179 [PubMed - indexed for MEDLINE]Related articles

Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein inhibitor.

Kuo GH, Rano T, Pelton P, Demarest KT, Gibbs AC, Murray WV, Damiano BP, Connelly MA.

J Med Chem. 2009 Mar 26;52(6):1768-72.PMID: 19236017 [PubMed - indexed for MEDLINE]Related articles

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. Epub 2008 Jun 7.PMID: 18599033 [PubMed - indexed for MEDLINE]Related articles

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 [PubMed - indexed for MEDLINE]Related articles

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 [PubMed - indexed for MEDLINE]Related articles

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 [PubMed - indexed for MEDLINE]Related articles

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 [PubMed - indexed for MEDLINE]Related articles

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 [PubMed - indexed for MEDLINE]Related articles

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 [PubMed - indexed for MEDLINE]Related articles

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 [PubMed - indexed for MEDLINE]Related articles

Indole-glucosides as novel sodium glucose co-transporter 2 (SGLT2) inhibitors. Part 2.

Zhang X, Urbanski M, Patel M, Cox GG, Zeck RE, Bian H, Conway BR, Beavers MP, Rybczynski PJ, Demarest KT.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1696-701. Epub 2005 Dec 27.PMID: 16380256 [PubMed - indexed for MEDLINE]Related articles

Heteroaryl-O-glucosides as novel sodium glucose co-transporter 2 inhibitors. Part 1.

Zhang X, Urbanski M, Patel M, Zeck RE, Cox GG, Bian H, Conway BR, Pat Beavers M, Rybczynski PJ, Demarest KT.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5202-6. Epub 2005 Sep 28.PMID: 16198559 [PubMed - indexed for MEDLINE]Related articles

Distinctive and synergistic signaling of human adenosine A2a and dopamine D2L receptors in CHO cells.

Tang Y, Demarest KT.

J Recept Signal Transduct Res. 2005;25(3):159-79.PMID: 16194932 [PubMed - indexed for MEDLINE]Related articles

Synthesis and evaluation of 3-anilino-quinoxalinones as glycogen phosphorylase inhibitors.

Dudash J Jr, Zhang Y, Moore JB, Look R, Liang Y, Beavers MP, Conway BR, Rybczynski PJ, Demarest KT.

Bioorg Med Chem Lett. 2005 Nov 1;15(21):4790-3.PMID: 16143521 [PubMed - indexed for MEDLINE]Related articles

Sustained aquaretic effect of the V2-AVP receptor antagonist, RWJ-351647, in cirrhotic rats with ascites and water retention.

Ros J, Fernández-Varo G, Muñoz-Luque J, Arroyo V, Rodés J, Gunnet JW, Demarest KT, Jiménez W.

Br J Pharmacol. 2005 Nov;146(5):654-61.PMID: 16113688 [PubMed - indexed for MEDLINE]Related articlesFree article

Pharmacological profile of a novel, non-TZD PPARgamma agonist.

Chen X, Osborne MC, Rybczynski PJ, Zeck R, Yang M, Xu J, Zhou L, Cryan E, Tang Y, Demarest KT.

Diabetes Obes Metab. 2005 Sep;7(5):536-46.PMID: 16050946 [PubMed - indexed for MEDLINE]Related articles

Nuclear receptors as potential targets for modulating reverse cholesterol transport.

Pelton PD, Patel M, Demarest KT.

Curr Top Med Chem. 2005;5(3):265-82. Review.PMID: 15857310 [PubMed - indexed for MEDLINE]Related articles

Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.

Zhang HC, Derian CK, McComsey DF, White KB, Ye H, Hecker LR, Li J, Addo MF, Croll D, Eckardt AJ, Smith CE, Li Q, Cheung WM, Conway BR, Emanuel S, Demarest KT, Andrade-Gordon P, Damiano BP, Maryanoff BE.

J Med Chem. 2005 Mar 24;48(6):1725-8.PMID: 15771419 [PubMed - indexed for MEDLINE]Related articles

Topiramate is an insulin-sensitizing compound in vivo with direct effects on adipocytes in female ZDF rats.

Wilkes JJ, Nelson E, Osborne M, Demarest KT, Olefsky JM.

Am J Physiol Endocrinol Metab. 2005 Mar;288(3):E617-24. Epub 2004 Nov 9.PMID: 15536205 [PubMed - indexed for MEDLINE]Related articlesFree article

Glycosylated dihydrochalcones as potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitors.

Dudash J Jr, Zhang X, Zeck RE, Johnson SG, Cox GG, Conway BR, Rybczynski PJ, Demarest KT.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5121-5.PMID: 15380212 [PubMed - indexed for MEDLINE]Related articles

Development of a sensitive and HTS-compatible reporter gene assay for functional analysis of human adenosine A2a receptors in CHO-K1 cells.

Tang Y, Luo J, Fleming CR, Kong Y, Olini GC Jr, Wildey MJ, Cavender DE, Demarest KT.

Assay Drug Dev Technol. 2004 Jun;2(3):281-9.PMID: 15285909 [PubMed - indexed for MEDLINE]Related articles

Design, synthesis, and biological evaluation of novel 7-azaindolyl-heteroaryl-maleimides as potent and selective glycogen synthase kinase-3beta (GSK-3beta) inhibitors.

O'Neill DJ, Shen L, Prouty C, Conway BR, Westover L, Xu JZ, Zhang HC, Maryanoff BE, Murray WV, Demarest KT, Kuo GH.

Bioorg Med Chem. 2004 Jun 15;12(12):3167-85.PMID: 15158785 [PubMed - indexed for MEDLINE]Related articles

3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.

Zhang HC, Ye H, Conway BR, Derian CK, Addo MF, Kuo GH, Hecker LR, Croll DR, Li J, Westover L, Xu JZ, Look R, Demarest KT, Andrade-Gordon P, Damiano BP, Maryanoff BE.

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3245-50.PMID: 15149684 [PubMed - indexed for MEDLINE]Related articles

Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists.

Xiang MA, Chen RH, Demarest KT, Gunnet J, Look R, Hageman W, Murray WV, Combs DW, Rybczynski PJ, Patel M.

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3143-6.PMID: 15149662 [PubMed - indexed for MEDLINE]Related articles

Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists.

Xiang MA, Chen RH, Demarest KT, Gunnet J, Look R, Hageman W, Murray WV, Combs DW, Patel M.

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2987-9.PMID: 15125974 [PubMed - indexed for MEDLINE]Related articles

Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.

Matthews JM, Hoekstra WJ, Dyatkin AB, Hecker LR, Hlasta DJ, Poulter BL, Andrade-Gordon P, de Garavilla L, Demarest KT, Ericson E, Gunnet JW, Hageman W, Look R, Moore JB, Reynolds CH, Maryanoff BE.

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2747-52.PMID: 15125926 [PubMed - indexed for MEDLINE]Related articles

Synthesis and biological evaluation of novel macrocyclic bis-7-azaindolylmaleimides as potent and highly selective glycogen synthase kinase-3 beta (GSK-3 beta) inhibitors.

Shen L, Prouty C, Conway BR, Westover L, Xu JZ, Look RA, Chen X, Beavers MP, Roberts J, Murray WV, Demarest KT, Kuo GH.

Bioorg Med Chem. 2004 Mar 1;12(5):1239-55.PMID: 14980636 [PubMed - indexed for MEDLINE]Related articles

Reduction in glucagon receptor expression by an antisense oligonucleotide ameliorates diabetic syndrome in db/db mice.

Liang Y, Osborne MC, Monia BP, Bhanot S, Gaarde WA, Reed C, She P, Jetton TL, Demarest KT.

Diabetes. 2004 Feb;53(2):410-7.PMID: 14747292 [PubMed - indexed for MEDLINE]Related articlesFree article

Benzoxazinones as PPARgamma agonists. 2. SAR of the amide substituent and in vivo results in a type 2 diabetes model.

Rybczynski PJ, Zeck RE, Dudash J Jr, Combs DW, Burris TP, Yang M, Osborne MC, Chen X, Demarest KT.

J Med Chem. 2004 Jan 1;47(1):196-209.PMID: 14695833 [PubMed - indexed for MEDLINE]Related articles

2,5-disubstituted 3,4-dihydro-2H-benzo[b][1,4]thiazepines as potent and selective V2 arginine vasopressin receptor antagonists.

Urbanski MJ, Chen RH, Demarest KT, Gunnet J, Look R, Ericson E, Murray WV, Rybczynski PJ, Zhang X.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):4031-4.PMID: 14592501 [PubMed - indexed for MEDLINE]Related articles

Validation of a cell-based screen for insulin receptor modulators by quantification of insulin receptor phosphorylation.

Minor LK, Westover L, Kong Y, Patel D, Wildey MJ, Conway BR, Demarest KT.

J Biomol Screen. 2003 Aug;8(4):439-46.PMID: 14567796 [PubMed - indexed for MEDLINE]Related articles

Human cardiomyocytes express high level of Na+/glucose cotransporter 1 (SGLT1).

Zhou L, Cryan EV, D'Andrea MR, Belkowski S, Conway BR, Demarest KT.

J Cell Biochem. 2003 Oct 1;90(2):339-46.PMID: 14505350 [PubMed - indexed for MEDLINE]Related articles

Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.

Kuo GH, Prouty C, DeAngelis A, Shen L, O'Neill DJ, Shah C, Connolly PJ, Murray WV, Conway BR, Cheung P, Westover L, Xu JZ, Look RA, Demarest KT, Emanuel S, Middleton SA, Jolliffe L, Beavers MP, Chen X.

J Med Chem. 2003 Sep 11;46(19):4021-31.PMID: 12954055 [PubMed - indexed for MEDLINE]Related articles

Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.

Zhang HC, White KB, Ye H, McComsey DF, Derian CK, Addo MF, Andrade-Gordon P, Eckardt AJ, Conway BR, Westover L, Xu JZ, Look R, Demarest KT, Emanuel S, Maryanoff BE.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3049-53.PMID: 12941331 [PubMed - indexed for MEDLINE]Related articles

Benzoxazinones as PPARgamma agonists. part 1: SAR of three aromatic regions.

Rybczynski PJ, Zeck RE, Combs DW, Turchi I, Burris TP, Xu JZ, Yang M, Demarest KT.

Bioorg Med Chem Lett. 2003 Jul 21;13(14):2359-62.PMID: 12824034 [PubMed - indexed for MEDLINE]Related articles

The use of biosensors to study GPCR function: applications for high-content screening.

Conway BR, Demarest KT.

Receptors Channels. 2002;8(5-6):331-41. Review.PMID: 12690960 [PubMed - indexed for MEDLINE]Related articles

Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.

Matthews JM, Greco MN, Hecker LR, Hoekstra WJ, Andrade-Gordon P, de Garavilla L, Demarest KT, Ericson E, Gunnet JW, Hageman W, Look R, Moore JB, Maryanoff BE.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):753-6.PMID: 12639574 [PubMed - indexed for MEDLINE]Related articles

Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.

Dyatkin AB, Hoekstra WJ, Hlasta DJ, Andrade-Gordon P, de Garavilla L, Demarest KT, Gunnet JW, Hageman W, Look R, Maryanoff BE.

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3081-4. Erratum in: Bioorg Med Chem Lett. 2004 Jun 21;14(12):3363. PMID: 12372506 [PubMed - indexed for MEDLINE]Related articles

Quantitative analysis of agonist-dependent parathyroid hormone receptor trafficking in whole cells using a functional green fluorescent protein conjugate.

Conway BR, Minor LK, Xu JZ, D'Andrea MR, Ghosh RN, Demarest KT.

J Cell Physiol. 2001 Dec;189(3):341-55.PMID: 11748592 [PubMed - indexed for MEDLINE]Related articles

Discovery of the first non-peptide antagonist of the motilin receptor.

Beavers MP, Gunnet JW, Hageman W, Miller W, Moore JB, Zhou L, Chen RH, Xiang A, Urbanski M, Combs DW, Mayo KH, Demarest KT.

Drug Des Discov. 2001;17(3):243-51.PMID: 11469754 [PubMed - indexed for MEDLINE]Related articles

Cell-based, high-content screen for receptor internalization, recycling and intracellular trafficking.

Ghosh RN, Chen YT, DeBiasio R, DeBiasio RL, Conway BR, Minor LK, Demarest KT.

Biotechniques. 2000 Jul;29(1):170-5.PMID: 10907092 [PubMed - indexed for MEDLINE]Related articles

A branched DNA signal amplification assay to quantitate messenger RNA of human uncoupling proteins 1, 2, and 3.

Zhou L, Cryan EV, Minor LK, Gunnet JW, Demarest KT.

Anal Biochem. 2000 Jun 15;282(1):46-53.PMID: 10860498 [PubMed - indexed for MEDLINE]Related articles

Quantification of G-Protein Coupled Receptor Internatilization Using G-Protein Coupled Receptor-Green Fluorescent Protein Conjugates with the ArrayScantrade mark High-Content Screening System.

Conway BR, Minor LK, Xu JZ, Gunnet JW, DeBiasio R, D'Andrea MR, Rubin R, DeBiasio R, Giuliano K, DeBiasio L, Demarest KT.

J Biomol Screen. 1999;4(2):75-86.PMID: 10838415 [PubMed - as supplied by publisher]Related articles

Characterization of the progestin receptors in the human TE85 and murine MC3T3-E1 osteoblast-like cell lines.

Gunnet JW, Granger K, Cryan E, Demarest KT.

J Endocrinol. 1999 Oct;163(1):139-47.PMID: 10495416 [PubMed - indexed for MEDLINE]Related articlesFree article

PPARgamma activation induces the expression of the adipocyte fatty acid binding protein gene in human monocytes.

Pelton PD, Zhou L, Demarest KT, Burris TP.

Biochem Biophys Res Commun. 1999 Aug 2;261(2):456-8.PMID: 10425206 [PubMed - indexed for MEDLINE]Related articles

A novel method for analysis of nuclear receptor function at natural promoters: peroxisome proliferator-activated receptor gamma agonist actions on aP2 gene expression detected using branched DNA messenger RNA quantitation.

Burris TP, Pelton PD, Zhou L, Osborne MC, Cryan E, Demarest KT.

Mol Endocrinol. 1999 Mar;13(3):410-7.PMID: 10076998 [PubMed - indexed for MEDLINE]Related articlesFree article

Nonsteroidal progesterone receptor ligands. 2. High-affinity ligands with selectivity for bone cell progesterone receptors.

Combs DW, Reese K, Cornelius LA, Gunnet JW, Cryan EV, Granger KS, Jordan JJ, Demarest KT.

J Med Chem. 1995 Dec 8;38(25):4880-4.PMID: 8523400 [PubMed - indexed for MEDLINE]Related articles

Development of a heterologous radioimmunoassay for canine osteocalcin.

Wang SP, Demarest KT, Gunnet JW, Baylink DJ, Lau KH.

Calcif Tissue Int. 1994 Aug;55(2):134-40.PMID: 7953979 [PubMed - indexed for MEDLINE]Related articles

Picomolar norethindrone in vitro stimulates the cell proliferation and activity of a human osteosarcoma cell line and increases bone collagen synthesis without an effect on bone resorption.

Lau KH, Wang SP, Linkhart TA, Demarest KT, Baylink DJ.

J Bone Miner Res. 1994 May;9(5):695-703.PMID: 8053399 [PubMed - indexed for MEDLINE]Related articles

Maternal and fetal cardiovascular effects and placental transfer of the oxytocin antagonist atosiban in late-gestation pregnant sheep.

Greig PC, Massmann GA, Demarest KT, Weglein RC, Holland ML, Figueroa JP.

Am J Obstet Gynecol. 1993 Oct;169(4):897-902.PMID: 8238146 [PubMed - indexed for MEDLINE]Related articles