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Items: 38

1.

Inhibition of bone resorption by the cathepsin K inhibitor odanacatib is fully reversible.

Zhuo Y, Gauthier JY, Black WC, Percival MD, Duong LT.

Bone. 2014 Oct;67:269-80. doi: 10.1016/j.bone.2014.07.013. Epub 2014 Jul 16.

PMID:
25038310
2.

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
3.

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
4.

Lack of cathepsin activities alter or prevent the development of lung granulomas in a mouse model of sarcoidosis.

Samokhin AO, Gauthier JY, Percival MD, Brömme D.

Respir Res. 2011 Jan 20;12:13. doi: 10.1186/1465-9921-12-13.

5.

Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.

Isabel E, Mellon C, Boyd MJ, Chauret N, Deschênes D, Desmarais S, Falgueyret JP, Gauthier JY, Khougaz K, Lau CK, Léger S, Levorse DA, Li CS, Massé F, Percival MD, Roy B, Scheigetz J, Thérien M, Truong VL, Wesolowski G, Young RN, Zamboni R, Black WC.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):920-3. doi: 10.1016/j.bmcl.2010.12.070. Epub 2010 Dec 19.

PMID:
21232956
6.

Probing cathepsin S activity in whole blood by the activity-based probe BIL-DMK: cellular distribution in human leukocyte populations and evidence of diurnal modulation.

Veilleux A, Black WC, Gauthier JY, Mellon C, Percival MD, Tawa P, Falgueyret JP.

Anal Biochem. 2011 Apr 1;411(1):43-9. doi: 10.1016/j.ab.2010.11.022. Epub 2010 Nov 19.

PMID:
21094118
7.

Pharmacological and genetic evidence that cathepsin B is not the physiological activator of rodent prorenin.

Percival MD, Toulmond S, Coulombe N, Cromlish W, Desmarais S, Liu S, St-Jacques R, Gauthier JY, Fournier JF.

Biol Chem. 2010 Dec;391(12):1469-73. doi: 10.1515/BC.2010.140.

PMID:
20868234
8.

Genetic and pharmacological evaluation of cathepsin s in a mouse model of asthma.

Deschamps K, Cromlish W, Weicker S, Lamontagne S, Huszar SL, Gauthier JY, Mudgett JS, Guimond A, Romand R, Frossard N, Percival MD, Slipetz D, Tan CM.

Am J Respir Cell Mol Biol. 2011 Jul;45(1):81-7. doi: 10.1165/rcmb.2009-0392OC. Epub 2010 Sep 20.

PMID:
20855652
9.

Cathepsin K inhibitors prevent bone loss in estrogen-deficient rabbits.

Pennypacker BL, Duong LT, Cusick TE, Masarachia PJ, Gentile MA, Gauthier JY, Black WC, Scott BB, Samadfam R, Smith SY, Kimmel DB.

J Bone Miner Res. 2011 Feb;26(2):252-62. doi: 10.1002/jbmr.223.

10.

Pharmacological inhibition of cathepsin S decreases atherosclerotic lesions in Apoe-/- mice.

Samokhin AO, Lythgo PA, Gauthier JY, Percival MD, Brömme D.

J Cardiovasc Pharmacol. 2010 Jul;56(1):98-105. doi: 10.1097/FJC.0b013e3181e23e10.

PMID:
20410833
11.

The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.

Isabel E, Bateman KP, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Gauthier JY, Lamontagne S, Lau CK, Léger S, LeRiche T, Lévesque JF, Li CS, Massé F, McKay DJ, Mellon C, Nicoll-Griffith DA, Oballa RM, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Wesolowski G, Young RN, Zamboni R, Black WC.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):887-92. doi: 10.1016/j.bmcl.2009.12.083. Epub 2009 Dec 28.

PMID:
20061146
12.

Selective isolation of in vitro phase II conjugates using a lipophilic anionic exchange solid phase extraction method.

Gagné S, Laterreur J, Mahrouche L, Sørensen D, Gauthier JY, Truong VL, Chauret N, Lévesque JF.

J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Mar 1;863(2):242-8. doi: 10.1016/j.jchromb.2008.01.032. Epub 2008 Jan 30.

PMID:
18262477
13.

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.

Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. doi: 10.1016/j.bmcl.2007.12.047. Epub 2008 Jan 15.

PMID:
18226527
14.

The identification of potent, selective, and bioavailable cathepsin S inhibitors.

Gauthier JY, Black WC, Courchesne I, Cromlish W, Desmarais S, Houle R, Lamontagne S, Li CS, Massé F, McKay DJ, Ouellet M, Robichaud J, Truchon JF, Truong VL, Wang Q, Percival MD.

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33. Epub 2007 Jun 10.

PMID:
17590332
15.

Identification of a potent and selective non-basic cathepsin K inhibitor.

Li CS, Deschenes D, Desmarais S, Falgueyret JP, Gauthier JY, Kimmel DB, Léger S, Massé F, McGrath ME, McKay DJ, Percival MD, Riendeau D, Rodan SB, Thérien M, Truong VL, Wesolowski G, Zamboni R, Black WC.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9. Epub 2006 Jan 18.

PMID:
16413777
16.

Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.

Lau CK, Bayly CI, Gauthier JY, Li CS, Therien M, Asante-Appiah E, Cromlish W, Boie Y, Forghani F, Desmarais S, Wang Q, Skorey K, Waddleton D, Payette P, Ramachandran C, Kennedy BP, Scapin G.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):1043-8.

PMID:
15013020
17.

Protein tyrosine phosphatase-1B dephosphorylation of the insulin receptor occurs in a perinuclear endosome compartment in human embryonic kidney 293 cells.

Romsicki Y, Reece M, Gauthier JY, Asante-Appiah E, Kennedy BP.

J Biol Chem. 2004 Mar 26;279(13):12868-75. Epub 2004 Jan 13.

18.

The structural basis for the selectivity of benzotriazole inhibitors of PTP1B.

Scapin G, Patel SB, Becker JW, Wang Q, Desponts C, Waddleton D, Skorey K, Cromlish W, Bayly C, Therien M, Gauthier JY, Li CS, Lau CK, Ramachandran C, Kennedy BP, Asante-Appiah E.

Biochemistry. 2003 Oct 7;42(39):11451-9.

PMID:
14516196
19.

Pyridazinones as selective cyclooxygenase-2 inhibitors.

Li CS, Brideau C, Chan CC, Savoie C, Claveau D, Charleson S, Gordon R, Greig G, Gauthier JY, Lau CK, Riendeau D, Thérien M, Wong E, Prasit P.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):597-600.

PMID:
12639538
20.

Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx).

Nicoll-Griffith DA, Yergey JA, Trimble LA, Silva JM, Li C, Chauret N, Gauthier JY, Grimm E, Léger S, Roy P, Thérien M, Wang Z, Prasit P, Zamboni R, Young RN, Brideau C, Chan CC, Mancini J, Riendeau D.

Bioorg Med Chem Lett. 2000 Dec 4;10(23):2683-6.

PMID:
11128651
21.

Description of a 96-well plate assay to measure cytochrome P4503A inhibition in human liver microsomes using a selective fluorescent probe.

Chauret N, Tremblay N, Lackman RL, Gauthier JY, Silva JM, Marois J, Yergey JA, Nicoll-Griffith DA.

Anal Biochem. 1999 Dec 15;276(2):215-26.

PMID:
10603245
22.

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
23.

A new structural variation on the methanesulfonylphenyl class of selective cyclooxygenase-2 inhibitors.

Li CS, Black WC, Brideau C, Chan CC, Charleson S, Cromlish WA, Claveau D, Gauthier JY, Gordon R, Greig G, Grimm E, Guay J, Lau CK, Riendeau D, Thérien M, Visco DM, Wong E, Xu L, Prasit P.

Bioorg Med Chem Lett. 1999 Nov 15;9(22):3181-6.

PMID:
10576684
24.

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
25.

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
26.

2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.

Friesen RW, Brideau C, Chan CC, Charleson S, Deschênes D, Dubé D, Ethier D, Fortin R, Gauthier JY, Girard Y, Gordon R, Greig GM, Riendeau D, Savoie C, Wang Z, Wong E, Visco D, Xu LJ, Young RN.

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2777-82.

PMID:
9873621
27.

A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.

Guay D, Gauthier JY, Dufresne C, Jones TR, McAuliffe M, McFarlane C, Metters KM, Prasit P, Rochette C, Roy P, Sawyer N, Zamboni R.

Bioorg Med Chem Lett. 1998 Mar 3;8(5):453-8.

PMID:
9871597
28.

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
29.

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
30.

Pharmacology of montelukast sodium (Singulair), a potent and selective leukotriene D4 receptor antagonist.

Jones TR, Labelle M, Belley M, Champion E, Charette L, Evans J, Ford-Hutchinson AW, Gauthier JY, Lord A, Masson P, et al.

Can J Physiol Pharmacol. 1995 Feb;73(2):191-201. Erratum in: Can J Physiol Pharmacol 1995 Jun;73(6):747.

PMID:
7621356
31.

A new class of leukotriene biosynthesis inhibitor: the development of MK-0591.

Prasit P, Belley M, Blouin M, Brideau C, Chan C, Charleson S, Evans JF, Frenette R, Gauthier JY, Guay J, et al.

J Lipid Mediat. 1993 Mar-Apr;6(1-3):239-44.

PMID:
8357985
33.

Pharmacology of the leukotriene antagonist verlukast: the (R)-enantiomer of MK-571.

Jones TR, Zamboni R, Belley M, Champion E, Charette L, Ford-Hutchinson AW, Gauthier JY, Leger S, Lord A, Masson P, et al.

Can J Physiol Pharmacol. 1991 Dec;69(12):1847-54.

PMID:
1666333
34.

5-Lipoxygenase-activating protein is the target of a quinoline class of leukotriene synthesis inhibitors.

Evans JF, Lévillé C, Mancini JA, Prasit P, Thérien M, Zamboni R, Gauthier JY, Fortin R, Charleson P, MacIntyre DE, et al.

Mol Pharmacol. 1991 Jul;40(1):22-7.

PMID:
1857337
36.

Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist.

Jones TR, Zamboni R, Belley M, Champion E, Charette L, Ford-Hutchinson AW, Frenette R, Gauthier JY, Leger S, Masson P, et al.

Can J Physiol Pharmacol. 1989 Jan;67(1):17-28.

PMID:
2540892
37.

Design and synthesis of sodium (beta R*, gamma S*)-4-[[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl] thio]-gamma-hydroxy-beta-methylbenzenebutanoate: a novel, selective, and orally active receptor antagonist of leukotriene D4.

Young RN, Bélanger P, Champion E, DeHaven RN, Denis D, Ford-Hutchinson AW, Fortin R, Frenette R, Gauthier JY, Gillard J, et al.

J Med Chem. 1986 Sep;29(9):1573-6. No abstract available.

PMID:
3746809
38.

L-649,923, sodium (beta S*, gamma R*)-4-(3-(4-acetyl-3-hydroxy-2-propylphenoxy)-propylthio)- gamma-hydroxy-beta-methylbenzenebutanoate, a selective, orally active leukotriene receptor antagonist.

Jones TR, Young R, Champion E, Charette L, Denis D, Ford-Hutchinson AW, Frenette R, Gauthier JY, Guindon Y, Kakushima M, et al.

Can J Physiol Pharmacol. 1986 Aug;64(8):1068-75.

PMID:
3024787

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