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Items: 1 to 50 of 58

1.

Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells.

Mullarky E, Xu J, Robin AD, Huggins DJ, Jennings A, Noguchi N, Olland A, Lakshminarasimhan D, Miller M, Tomita D, Michino M, Su T, Zhang G, Stamford AW, Meinke PT, Kargman S, Cantley LC.

Bioorg Med Chem Lett. 2019 Sep 1;29(17):2503-2510. doi: 10.1016/j.bmcl.2019.07.011. Epub 2019 Jul 6.

PMID:
31327531
2.

Antibacterial small molecules targeting the conserved TOPRIM domain of DNA gyrase.

Walker SS, Labroli M, Painter RE, Wiltsie J, Sherborne B, Murgolo N, Sher X, Mann P, Zuck P, Garlisi CG, Su J, Kargman S, Xiao L, Scapin G, Salowe S, Devito K, Sheth P, Buist N, Tan CM, Black TA, Roemer T.

PLoS One. 2017 Jul 10;12(7):e0180965. doi: 10.1371/journal.pone.0180965. eCollection 2017.

3.

Discovery of MK-8831, A Novel Spiro-Proline Macrocycle as a Pan-Genotypic HCV-NS3/4a Protease Inhibitor.

Neelamkavil SF, Agrawal S, Bara T, Bennett C, Bhat S, Biswas D, Brockunier L, Buist N, Burnette D, Cartwright M, Chackalamannil S, Chase R, Chelliah M, Chen A, Clasby M, Colandrea VJ, Davies IW, Eagen K, Guo Z, Han Y, Howe J, Jayne C, Josien H, Kargman S, Marcantonio K, Miao S, Miller R, Nolting A, Pinto P, Rajagopalan M, Ruck RT, Shah U, Soriano A, Sperbeck D, Velazquez F, Wu J, Xia Y, Venkatraman S.

ACS Med Chem Lett. 2015 Dec 22;7(1):111-6. doi: 10.1021/acsmedchemlett.5b00425. eCollection 2016 Jan 14.

4.

Stearoyl-CoA desaturase inhibition blocks formation of hepatitis C virus-induced specialized membranes.

Lyn RK, Singaravelu R, Kargman S, O'Hara S, Chan H, Oballa R, Huang Z, Jones DM, Ridsdale A, Russell RS, Partridge AW, Pezacki JP.

Sci Rep. 2014 Apr 1;4:4549. doi: 10.1038/srep04549.

5.

Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity.

Coburn CA, Meinke PT, Chang W, Fandozzi CM, Graham DJ, Hu B, Huang Q, Kargman S, Kozlowski J, Liu R, McCauley JA, Nomeir AA, Soll RM, Vacca JP, Wang D, Wu H, Zhong B, Olsen DB, Ludmerer SW.

ChemMedChem. 2013 Dec;8(12):1930-40. doi: 10.1002/cmdc.201300343. Epub 2013 Oct 14.

PMID:
24127258
6.

Murgocil is a highly bioactive staphylococcal-specific inhibitor of the peptidoglycan glycosyltransferase enzyme MurG.

Mann PA, Müller A, Xiao L, Pereira PM, Yang C, Ho Lee S, Wang H, Trzeciak J, Schneeweis J, Dos Santos MM, Murgolo N, She X, Gill C, Balibar CJ, Labroli M, Su J, Flattery A, Sherborne B, Maier R, Tan CM, Black T, Onder K, Kargman S, Monsma FJ Jr, Pinho MG, Schneider T, Roemer T.

ACS Chem Biol. 2013 Nov 15;8(11):2442-51. doi: 10.1021/cb400487f. Epub 2013 Sep 5.

PMID:
23957438
7.

Discovery of novel P2Y14 agonist and antagonist using conventional and nonconventional methods.

Hamel M, Henault M, Hyjazie H, Morin N, Bayly C, Skorey K, Therien AG, Mancini J, Brideau C, Kargman S.

J Biomol Screen. 2011 Oct;16(9):1098-105. doi: 10.1177/1087057111415525. Epub 2011 Aug 5.

PMID:
21821827
8.

Applying the pro-drug approach to afford highly bioavailable antagonists of P2Y(14).

Robichaud J, Fournier JF, Gagné S, Gauthier JY, Hamel M, Han Y, Hénault M, Kargman S, Levesque JF, Mamane Y, Mancini J, Morin N, Mulrooney E, Wu J, Black WC.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4366-8. doi: 10.1016/j.bmcl.2010.12.113. Epub 2010 Dec 28.

PMID:
21689930
9.

Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists.

Guay D, Beaulieu C, Belley M, Crane SN, DeLuca J, Gareau Y, Hamel M, Henault M, Hyjazie H, Kargman S, Chan CC, Xu L, Gordon R, Li L, Mamane Y, Morin N, Mancini J, Thérien M, Tranmer G, Truong VL, Wang Z, Black WC.

Bioorg Med Chem Lett. 2011 May 15;21(10):2832-5. doi: 10.1016/j.bmcl.2011.03.084. Epub 2011 Mar 30.

PMID:
21507642
10.

The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14.

Gauthier JY, Belley M, Deschênes D, Fournier JF, Gagné S, Gareau Y, Hamel M, Hénault M, Hyjazie H, Kargman S, Lavallée G, Levesque JF, Li L, Mamane Y, Mancini J, Morin N, Mulrooney E, Robichaud J, Thérien M, Tranmer G, Wang Z, Wu J, Black WC.

Bioorg Med Chem Lett. 2011 May 15;21(10):2836-9. doi: 10.1016/j.bmcl.2011.03.081. Epub 2011 Mar 31.

PMID:
21507640
11.

Design, synthesis, and evaluation of novel 3-amino-4-hydrazine-cyclobut-3-ene-1,2-diones as potent and selective CXCR2 chemokine receptor antagonists.

Liu S, Liu Y, Wang H, Ding Y, Wu H, Dong J, Wong A, Chen SH, Li G, Chan M, Sawyer N, Gervais FG, Henault M, Kargman S, Bedard LL, Han Y, Friesen R, Lobell RB, Stout DM.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5741-5. doi: 10.1016/j.bmcl.2009.08.014. Epub 2009 Aug 7.

PMID:
19713110
12.

Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).

Sturino CF, O'Neill G, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N, Aubin Y, Bateman KP, Chauret N, Day SH, Lévesque JF, Seto C, Silva JH, Trimble LA, Carriere MC, Denis D, Greig G, Kargman S, Lamontagne S, Mathieu MC, Sawyer N, Slipetz D, Abraham WM, Jones T, McAuliffe M, Piechuta H, Nicoll-Griffith DA, Wang Z, Zamboni R, Young RN, Metters KM.

J Med Chem. 2007 Feb 22;50(4):794-806.

PMID:
17300164
13.

Identification of an indole series of prostaglandin D2 receptor antagonists.

Sturino CF, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N, Brideau C, Cauchon E, Carriere MC, Denis D, Greig G, Kargman S, Lamontagne S, Mathieu MC, Sawyer N, Slipetz D, O'Neill G, Wang Z, Zamboni R, Metters KM, Young RN.

Bioorg Med Chem Lett. 2006 Jun 1;16(11):3043-8. Epub 2006 Mar 10.

PMID:
16529930
14.

The C3a receptor antagonist SB 290157 has agonist activity.

Mathieu MC, Sawyer N, Greig GM, Hamel M, Kargman S, Ducharme Y, Lau CK, Friesen RW, O'Neill GP, Gervais FG, Therien AG.

Immunol Lett. 2005 Sep 15;100(2):139-45. Epub 2005 Mar 25.

PMID:
16154494
15.

Gob-5 is not essential for mucus overproduction in preclinical murine models of allergic asthma.

Robichaud A, Tuck SA, Kargman S, Tam J, Wong E, Abramovitz M, Mortimer JR, Burston HE, Masson P, Hirota J, Slipetz D, Kennedy B, O'Neill G, Xanthoudakis S.

Am J Respir Cell Mol Biol. 2005 Sep;33(3):303-14. Epub 2005 Jun 9. Erratum in: Am J Respir Cell Mol Biol. 2006 Mar;34(3):383. Mortimer, James [corrected to Mortimer, James R].

PMID:
15947424
16.

2,3-Diarylthiophenes as selective EP1 receptor antagonists.

Ducharme Y, Blouin M, Carrière MC, Chateauneuf A, Côté B, Denis D, Frenette R, Greig G, Kargman S, Lamontagne S, Martins E, Nantel F, O'Neill G, Sawyer N, Metters KM, Friesen RW.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1155-60.

PMID:
15686932
17.

Cancer and cyclooxygenase-2 (COX-2) inhibition.

Evans JF, Kargman SL.

Curr Pharm Des. 2004;10(6):627-34. Review.

PMID:
14965325
18.

Inhibition of cyclooxygenase-2 by rofecoxib attenuates the growth and metastatic potential of colorectal carcinoma in mice.

Yao M, Kargman S, Lam EC, Kelly CR, Zheng Y, Luk P, Kwong E, Evans JF, Wolfe MM.

Cancer Res. 2003 Feb 1;63(3):586-92.

19.
20.

Maintenance of caspase-3 proenzyme dormancy by an intrinsic "safety catch" regulatory tripeptide.

Roy S, Bayly CI, Gareau Y, Houtzager VM, Kargman S, Keen SL, Rowland K, Seiden IM, Thornberry NA, Nicholson DW.

Proc Natl Acad Sci U S A. 2001 May 22;98(11):6132-7. Epub 2001 May 15.

21.

Chemoprevention of intestinal polyposis in the Apcdelta716 mouse by rofecoxib, a specific cyclooxygenase-2 inhibitor.

Oshima M, Murai N, Kargman S, Arguello M, Luk P, Kwong E, Taketo MM, Evans JF.

Cancer Res. 2001 Feb 15;61(4):1733-40.

22.

Expression of the cysteinyl leukotriene 1 receptor in normal human lung and peripheral blood leukocytes.

Figueroa DJ, Breyer RM, Defoe SK, Kargman S, Daugherty BL, Waldburger K, Liu Q, Clements M, Zeng Z, O'Neill GP, Jones TR, Lynch KR, Austin CP, Evans JF.

Am J Respir Crit Care Med. 2001 Jan;163(1):226-33.

PMID:
11208650
23.

Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.

Lau CK, Brideau C, Chan CC, Charleson S, Cromlish WA, Ethier D, Gauthier JY, Gordon R, Guay J, Kargman S, Li CS, Prasit P, Riendeau D, Thérien M, Visco DM, Xu L.

Bioorg Med Chem Lett. 1999 Nov 15;9(22):3187-92.

PMID:
10576685
24.

Characterization of the cloned guinea pig leukotriene B4 receptor: comparison to its human orthologue.

Boie Y, Stocco R, Sawyer N, Greig GM, Kargman S, Slipetz DM, O'Neill GP, Shimizu T, Yokomizo T, Metters KM, Abramovitz M.

Eur J Pharmacol. 1999 Sep 10;380(2-3):203-13.

PMID:
10513580
25.

Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles.

Chan CC, Boyce S, Brideau C, Charleson S, Cromlish W, Ethier D, Evans J, Ford-Hutchinson AW, Forrest MJ, Gauthier JY, Gordon R, Gresser M, Guay J, Kargman S, Kennedy B, Leblanc Y, Leger S, Mancini J, O'Neill GP, Ouellet M, Patrick D, Percival MD, Perrier H, Prasit P, Rodger I, et al.

J Pharmacol Exp Ther. 1999 Aug;290(2):551-60.

PMID:
10411562
26.

The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2-inhibitor.

Prasit P, Wang Z, Brideau C, Chan CC, Charleson S, Cromlish W, Ethier D, Evans JF, Ford-Hutchinson AW, Gauthier JY, Gordon R, Guay J, Gresser M, Kargman S, Kennedy B, Leblanc Y, Léger S, Mancini J, O'Neill GP, Ouellet M, Percival MD, Perrier H, Riendeau D, Rodger I, Zamboni R, et al.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1773-8.

PMID:
10406640
27.

Characterization of the human cysteinyl leukotriene CysLT1 receptor.

Lynch KR, O'Neill GP, Liu Q, Im DS, Sawyer N, Metters KM, Coulombe N, Abramovitz M, Figueroa DJ, Zeng Z, Connolly BM, Bai C, Austin CP, Chateauneuf A, Stocco R, Greig GM, Kargman S, Hooks SB, Hosfield E, Williams DL Jr, Ford-Hutchinson AW, Caskey CT, Evans JF.

Nature. 1999 Jun 24;399(6738):789-93.

PMID:
10391245
28.

Receptor for motilin identified in the human gastrointestinal system.

Feighner SD, Tan CP, McKee KK, Palyha OC, Hreniuk DL, Pong SS, Austin CP, Figueroa D, MacNeil D, Cascieri MA, Nargund R, Bakshi R, Abramovitz M, Stocco R, Kargman S, O'Neill G, Van Der Ploeg LH, Evans J, Patchett AA, Smith RG, Howard AD.

Science. 1999 Jun 25;284(5423):2184-8.

29.

Cloning of a novel G-protein-coupled receptor GPR 51 resembling GABAB receptors expressed predominantly in nervous tissues and mapped proximal to the hereditary sensory neuropathy type 1 locus on chromosome 9.

Ng GY, McDonald T, Bonnert T, Rigby M, Heavens R, Whiting P, Chateauneuf A, Coulombe N, Kargman S, Caskey T, Evans J, O'neill GP, Liu Q.

Genomics. 1999 Mar 15;56(3):288-95.

PMID:
10087195
30.

Identification of a GABAB receptor subunit, gb2, required for functional GABAB receptor activity.

Ng GY, Clark J, Coulombe N, Ethier N, Hebert TE, Sullivan R, Kargman S, Chateauneuf A, Tsukamoto N, McDonald T, Whiting P, Mezey E, Johnson MP, Liu Q, Kolakowski LF Jr, Evans JF, Bonner TI, O'Neill GP.

J Biol Chem. 1999 Mar 19;274(12):7607-10.

31.

Molecular characterization and expression of cloned human galanin receptors GALR2 and GALR3.

Kolakowski LF Jr, O'Neill GP, Howard AD, Broussard SR, Sullivan KA, Feighner SD, Sawzdargo M, Nguyen T, Kargman S, Shiao LL, Hreniuk DL, Tan CP, Evans J, Abramovitz M, Chateauneuf A, Coulombe N, Ng G, Johnson MP, Tharian A, Khoshbouei H, George SR, Smith RG, O'Dowd BF.

J Neurochem. 1998 Dec;71(6):2239-51.

32.

Cytosolic phospholipase A2, cyclo-oxygenases and arachidonate in human stomach tumours.

Soydan AS, Gaffen JD, Weech PK, Tremblay NM, Kargman S, O'Neill G, Bennett A, Tavares IA.

Eur J Cancer. 1997 Aug;33(9):1508-12.

PMID:
9337697
33.

Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor.

Riendeau D, Percival MD, Boyce S, Brideau C, Charleson S, Cromlish W, Ethier D, Evans J, Falgueyret JP, Ford-Hutchinson AW, Gordon R, Greig G, Gresser M, Guay J, Kargman S, Léger S, Mancini JA, O'Neill G, Ouellet M, Rodger IW, Thérien M, Wang Z, Webb JK, Wong E, Chan CC, et al.

Br J Pharmacol. 1997 May;121(1):105-17.

34.

Investigation of human cyclooxygenase-2 glycosylation heterogeneity and protein expression in insect and mammalian cell expression systems.

Percival MD, Bastien L, Griffin PR, Kargman S, Ouellet M, O'Neill GP.

Protein Expr Purif. 1997 Apr;9(3):388-98.

PMID:
9126611
35.

Characterization of autocrine inducible prostaglandin H synthase-2 (PGHS-2) in human osteosarcoma cells.

Wong E, DeLuca C, Boily C, Charleson S, Cromlish W, Denis D, Kargman S, Kennedy BP, Ouellet M, Skorey K, O'Neill GP, Vickers PJ, Riendeau D.

Inflamm Res. 1997 Feb;46(2):51-9.

PMID:
9085144
36.

From indomethacin to a selective COX-2 inhibitor. Development of indolalkanoic acids as potent and selective cyclooxygenase-2 inhibitors.

Lau CK, Black WC, Belley M, Chan C, Charleson S, Denis D, Gauthier JY, Gordon R, Guay D, Hamel P, Kargman S, Leblanc Y, Mancini J, Ouellet M, Percival D, Prasit P, Roy P, Skorey K, Tagari P, Vickers P, Wong E.

Adv Exp Med Biol. 1997;407:73-8. No abstract available.

PMID:
9321934
37.

Suppression of intestinal polyposis in Apc delta716 knockout mice by inhibition of cyclooxygenase 2 (COX-2).

Oshima M, Dinchuk JE, Kargman SL, Oshima H, Hancock B, Kwong E, Trzaskos JM, Evans JF, Taketo MM.

Cell. 1996 Nov 29;87(5):803-9.

38.

Mechanism of selective inhibition of human prostaglandin G/H synthase-1 and -2 in intact cells.

Kargman S, Wong E, Greig GM, Falgueyret JP, Cromlish W, Ethier D, Yergey JA, Riendeau D, Evans JF, Kennedy B, Tagari P, Francis DA, O'Neill GP.

Biochem Pharmacol. 1996 Oct 11;52(7):1113-25.

PMID:
8831731
39.

Characterization of Prostaglandin G/H Synthase 1 and 2 in rat, dog, monkey, and human gastrointestinal tracts.

Kargman S, Charleson S, Cartwright M, Frank J, Riendeau D, Mancini J, Evans J, O'Neill G.

Gastroenterology. 1996 Aug;111(2):445-54.

PMID:
8690211
40.

A human whole blood assay for clinical evaluation of biochemical efficacy of cyclooxygenase inhibitors.

Brideau C, Kargman S, Liu S, Dallob AL, Ehrich EW, Rodger IW, Chan CC.

Inflamm Res. 1996 Feb;45(2):68-74.

PMID:
8907587
41.

Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives.

Li CS, Black WC, Chan CC, Ford-Hutchinson AW, Gauthier JY, Gordon R, Guay D, Kargman S, Lau CK, Mancini J, et al.

J Med Chem. 1995 Dec 8;38(25):4897-905.

PMID:
8523403
42.

Thiopyranol[2,3,4-c,d]indoles as inhibitors of 5-lipoxygenase, 5-lipoxygenase-activating protein, and leukotriene C4 synthase.

Hutchinson JH, Charleson S, Evans JF, Falgueyret JP, Hoogsteen K, Jones TR, Kargman S, Macdonald D, McFarlane CS, Nicholson DW, et al.

J Med Chem. 1995 Oct 27;38(22):4538-47.

PMID:
7473582
43.

Expression of prostaglandin G/H synthase-1 and -2 protein in human colon cancer.

Kargman SL, O'Neill GP, Vickers PJ, Evans JF, Mancini JA, Jothy S.

Cancer Res. 1995 Jun 15;55(12):2556-9.

44.

Selective inhibitors of COX-2.

O'Neill GP, Kennedy BP, Mancini JA, Kargman S, Ouellet M, Yergey J, Falgueyret JP, Cromlish WA, Payette P, Chan CC, et al.

Agents Actions Suppl. 1995;46:159-68. Review.

PMID:
7610986
45.

Protein kinase C-dependent regulation of sulfidopeptide leukotriene biosynthesis and leukotriene C4 synthase in neutrophilic HL-60 cells.

Kargman S, Ali A, Vaillancourt JP, Evans JF, Nicholson DW.

Mol Pharmacol. 1994 May;45(5):1043-9.

PMID:
8190095
46.

Overexpression of human prostaglandin G/H synthase-1 and -2 by recombinant vaccinia virus: inhibition by nonsteroidal anti-inflammatory drugs and biosynthesis of 15-hydroxyeicosatetraenoic acid.

O'Neill GP, Mancini JA, Kargman S, Yergey J, Kwan MY, Falgueyret JP, Abramovitz M, Kennedy BP, Ouellet M, Cromlish W, et al.

Mol Pharmacol. 1994 Feb;45(2):245-54.

PMID:
8114674
47.

Leukotriene synthesis in U937 cells expressing recombinant 5-lipoxygenase.

Kargman S, Rousseau P, Reid GK, Rouzer CA, Mancini JA, Rands E, Dixon RA, Diehl RE, Léveillé C, Nathaniel D, et al.

J Lipid Mediat. 1993 May;7(1):31-45.

PMID:
8358023
48.

A23187-induced translocation of 5-lipoxygenase in osteosarcoma cells.

Kargman S, Vickers PJ, Evans JF.

J Cell Biol. 1992 Dec;119(6):1701-9.

49.

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