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Items: 1 to 50 of 72

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.

A fluorogenic near-infrared imaging agent for quantifying plasma and local tissue renin activity in vivo and ex vivo.

Zhang J, Preda DV, Vasquez KO, Morin J, Delaney J, Bao B, Percival MD, Xu D, McKay D, Klimas M, Bednar B, Sur C, Gao DZ, Madden K, Yared W, Rajopadhye M, Peterson JD.

Am J Physiol Renal Physiol. 2012 Aug 15;303(4):F593-603. doi: 10.1152/ajprenal.00361.2011. Epub 2012 Jun 6.

3.

Design and synthesis of potent, isoxazole-containing renin inhibitors.

Fournier PA, Arbour M, Cauchon E, Chen A, Chefson A, Ducharme Y, Falgueyret JP, Gagné S, Grimm E, Han Y, Houle R, Lacombe P, Lévesque JF, MacDonald D, Mackay B, McKay D, Percival MD, Ramtohul Y, St-Jacques R, Toulmond S.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2670-4. doi: 10.1016/j.bmcl.2012.03.014. Epub 2012 Mar 11.

PMID:
22450130
4.

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.

Chen A, Cauchon E, Chefson A, Dolman S, Ducharme Y, Dubé D, Falgueyret JP, Fournier PA, Gagné S, Gallant M, Grimm E, Han Y, Houle R, Huang JQ, Hughes G, Jûteau H, Lacombe P, Lauzon S, Lévesque JF, Liu S, Macdonald D, Mackay B, McKay D, Percival MD, St-Jacques R, Toulmond S.

Bioorg Med Chem Lett. 2011 Jul 1;21(13):3976-81. doi: 10.1016/j.bmcl.2011.05.014. Epub 2011 May 14.

PMID:
21641209
5.

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.

Chen A, Campeau LC, Cauchon E, Chefson A, Ducharme Y, Dubé D, Falgueyret JP, Fournier PA, Gagné S, Grimm E, Han Y, Houle R, Huang JQ, Lacombe P, Laliberté S, Lévesque JF, Liu S, MacDonald D, Mackay B, McKay D, Percival MD, Regan C, Regan H, St-Jacques R, Toulmond S.

Bioorg Med Chem Lett. 2011 Jul 1;21(13):3970-5. doi: 10.1016/j.bmcl.2011.05.013. Epub 2011 May 14.

PMID:
21621998
6.

Therapeutic dosing of an orally active, selective cathepsin S inhibitor suppresses disease in models of autoimmunity.

Baugh M, Black D, Westwood P, Kinghorn E, McGregor K, Bruin J, Hamilton W, Dempster M, Claxton C, Cai J, Bennett J, Long C, McKinnon H, Vink P, den Hoed L, Gorecka M, Vora K, Grant E, Percival MD, Boots AM, van Lierop MJ.

J Autoimmun. 2011 May;36(3-4):201-9. doi: 10.1016/j.jaut.2011.01.003. Epub 2011 Mar 24.

PMID:
21439785
7.

The discovery and synthesis of potent zwitterionic inhibitors of renin.

Aspiotis R, Chen A, Cauchon E, Dubé D, Falgueyret JP, Gagné S, Gallant M, Grimm EL, Houle R, Juteau H, Lacombe P, Laliberté S, Lévesque JF, MacDonald D, McKay D, Percival MD, Roy P, Soisson SM, Wu T.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2430-6. doi: 10.1016/j.bmcl.2011.02.067. Epub 2011 Feb 18.

PMID:
21429746
8.

Characterization of a stable, hypertensive rat model suitable for the consecutive evaluation of human renin inhibitors.

St-Jacques R, Toulmond S, Auger A, Binkert C, Cromlish W, Fischli W, Harris J, Hess P, Jie Lan, Liu S, Riendeau D, Steiner B, Percival MD.

J Renin Angiotensin Aldosterone Syst. 2011 Sep;12(3):133-45. doi: 10.1177/1470320310392618. Epub 2011 Mar 10.

PMID:
21393355
9.

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.

10.

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
11.

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
12.

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
13.

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
14.

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
15.

Therapeutic utility and medicinal chemistry of cathepsin C inhibitors.

Guay D, Beaulieu C, Percival MD.

Curr Top Med Chem. 2010;10(7):708-16. Review.

PMID:
20337582
16.

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
17.

Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools.

Desmarais S, Massé F, Percival MD.

Biol Chem. 2009 Sep;390(9):941-8. doi: 10.1515/BC.2009.092.

PMID:
19453281
18.

Renin and prorenin activate pathways implicated in organ damage in human mesangial cells independent of angiotensin II production.

Melnyk RA, Tam J, Boie Y, Kennedy BP, Percival MD.

Am J Nephrol. 2009;30(3):232-43. doi: 10.1159/000220260. Epub 2009 May 19.

PMID:
19451703
19.

Development of a homogeneous immunoassay for the detection of angiotensin I in plasma using AlphaLISA acceptor beads technology.

Cauchon E, Liu S, Percival MD, Rowland SE, Xu D, Binkert C, Strickner P, Falgueyret JP.

Anal Biochem. 2009 May 1;388(1):134-9. doi: 10.1016/j.ab.2009.02.031. Epub 2009 Mar 1.

PMID:
19258005
20.

Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis.

Robichaud J, Black WC, Thérien M, Paquet J, Oballa RM, Bayly CI, McKay DJ, Wang Q, Isabel E, Léger S, Mellon C, Kimmel DB, Wesolowski G, Percival MD, Massé F, Desmarais S, Falgueyret JP, Crane SN.

J Med Chem. 2008 Oct 23;51(20):6410-20. doi: 10.1021/jm800610j. Epub 2008 Sep 24.

PMID:
18811135
21.

Cleavage of type II collagen by cathepsin K in human osteoarthritic cartilage.

Dejica VM, Mort JS, Laverty S, Percival MD, Antoniou J, Zukor DJ, Poole AR.

Am J Pathol. 2008 Jul;173(1):161-9. doi: 10.2353/ajpath.2008.070494. Epub 2008 May 29.

22.

The type II collagen fragments Helix-II and CTX-II reveal different enzymatic pathways of human cartilage collagen degradation.

Charni-Ben Tabassi N, Desmarais S, Bay-Jensen AC, Delaissé JM, Percival MD, Garnero P.

Osteoarthritis Cartilage. 2008 Oct;16(10):1183-91. doi: 10.1016/j.joca.2008.02.008. Epub 2008 Apr 9.

23.

In vivo inhibition of serine protease processing requires a high fractional inhibition of cathepsin C.

Méthot N, Guay D, Rubin J, Ethier D, Ortega K, Wong S, Normandin D, Beaulieu C, Reddy TJ, Riendeau D, Percival MD.

Mol Pharmacol. 2008 Jun;73(6):1857-65. doi: 10.1124/mol.108.045682. Epub 2008 Mar 6.

PMID:
18326050
24.

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
25.

Effect of cathepsin k inhibitor basicity on in vivo off-target activities.

Desmarais S, Black WC, Oballa R, Lamontagne S, Riendeau D, Tawa P, Duong LT, Pickarski M, Percival MD.

Mol Pharmacol. 2008 Jan;73(1):147-56. Epub 2007 Oct 16.

PMID:
17940194
26.

Cathepsin K null mice show reduced adiposity during the rapid accumulation of fat stores.

Funicello M, Novelli M, Ragni M, Vottari T, Cocuzza C, Soriano-Lopez J, Chiellini C, Boschi F, Marzola P, Masiello P, Saftig P, Santini F, St-Jacques R, Desmarais S, Morin N, Mancini J, Percival MD, Pinchera A, Maffei M.

PLoS One. 2007 Aug 1;2(8):e683.

27.

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
28.

Primary amides as selective inhibitors of cathepsin K.

Léger S, Bayly CI, Black WC, Desmarais S, Falgueyret JP, Massé F, Percival MD, Truchon JF.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4328-32. Epub 2007 May 16.

PMID:
17544269
29.

Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.

Méthot N, Rubin J, Guay D, Beaulieu C, Ethier D, Reddy TJ, Riendeau D, Percival MD.

J Biol Chem. 2007 Jul 20;282(29):20836-46. Epub 2007 May 29.

30.

Beta-substituted cyclohexanecarboxamide cathepsin K inhibitors: modification of the 1,2-disubstituted aromatic core.

Robichaud J, Bayly CI, Black WC, Desmarais S, Léger S, Massé F, McKay DJ, Oballa RM, Pâquet J, Percival MD, Truchon JF, Wesolowski G, Crane SN.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3146-51. Epub 2007 Mar 15.

PMID:
17408953
31.

The consequences of lysosomotropism on the design of selective cathepsin K inhibitors.

Black WC, Percival MD.

Chembiochem. 2006 Oct;7(10):1525-35. Review.

PMID:
16921579
32.

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
33.

Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.

Falgueyret JP, Desmarais S, Oballa R, Black WC, Cromlish W, Khougaz K, Lamontagne S, Massé F, Riendeau D, Toulmond S, Percival MD.

J Med Chem. 2005 Dec 1;48(24):7535-43.

PMID:
16302795
34.

Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.

Palmer JT, Bryant C, Wang DX, Davis DE, Setti EL, Rydzewski RM, Venkatraman S, Tian ZQ, Burrill LC, Mendonca RV, Springman E, McCarter J, Chung T, Cheung H, Janc JW, McGrath M, Somoza JR, Enriquez P, Yu ZW, Strickley RM, Liu L, Venuti MC, Percival MD, Falgueyret JP, Prasit P, Oballa R, Riendeau D, Young RN, Wesolowski G, Rodan SB, Johnson C, Kimmel DB, Rodan G.

J Med Chem. 2005 Dec 1;48(24):7520-34.

PMID:
16302794
35.

Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.

Black WC, Bayly CI, Davis DE, Desmarais S, Falgueyret JP, Léger S, Li CS, Massé F, McKay DJ, Palmer JT, Percival MD, Robichaud J, Tsou N, Zamboni R.

Bioorg Med Chem Lett. 2005 Nov 1;15(21):4741-4.

PMID:
16154747
36.

An activity-based probe for the determination of cysteine cathepsin protease activities in whole cells.

Falgueyret JP, Black WC, Cromlish W, Desmarais S, Lamontagne S, Mellon C, Riendeau D, Rodan S, Tawa P, Wesolowski G, Bass KE, Venkatraman S, Percival MD.

Anal Biochem. 2004 Dec 15;335(2):218-27. Erratum in: Anal Biochem. 2005 May 15;340(2):380.

PMID:
15556560
37.

Aromatic hydroxamic acids and hydrazides as inhibitors of the peroxidase activity of prostaglandin H2 synthase-2.

Ouellet M, Aitken SM, English AM, Percival MD.

Arch Biochem Biophys. 2004 Nov 1;431(1):107-18.

PMID:
15464732
38.

Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.

Robichaud J, Bayly C, Oballa R, Prasit P, Mellon C, Falgueyret JP, Percival MD, Wesolowski G, Rodan SB.

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4291-5.

PMID:
15261289
39.

Quantitation of the lysosomotropic character of cationic amphiphilic drugs using the fluorescent basic amine Red DND-99.

Lemieux B, Percival MD, Falgueyret JP.

Anal Biochem. 2004 Apr 15;327(2):247-51.

PMID:
15051542
40.

Deletion of microsomal prostaglandin E2 (PGE2) synthase-1 reduces inducible and basal PGE2 production and alters the gastric prostanoid profile.

Boulet L, Ouellet M, Bateman KP, Ethier D, Percival MD, Riendeau D, Mancini JA, Méthot N.

J Biol Chem. 2004 May 28;279(22):23229-37. Epub 2004 Mar 11.

41.

Detergents profoundly affect inhibitor potencies against both cyclo-oxygenase isoforms.

Ouellet M, Falgueyret JP, Percival MD.

Biochem J. 2004 Feb 1;377(Pt 3):675-84.

42.

A novel class of nonpeptidic biaryl inhibitors of human cathepsin K.

Robichaud J, Oballa R, Prasit P, Falgueyret JP, Percival MD, Wesolowski G, Rodan SB, Kimmel D, Johnson C, Bryant C, Venkatraman S, Setti E, Mendonca R, Palmer JT.

J Med Chem. 2003 Aug 14;46(17):3709-27.

PMID:
12904076
43.
44.

Expression, purification and characterization of recombinant human microsomal PGE2 synthase-1.

Ouellet M, Pen A, Ear PH, Falgueyret JP, LeRiche TG, Mancini JA, Riendeau D, Percival MD.

Adv Exp Med Biol. 2003;525:113-6. No abstract available.

PMID:
12751747
45.

Purification and characterization of recombinant microsomal prostaglandin E synthase-1.

Ouellet M, Falgueyret JP, Ear PH, Pen A, Mancini JA, Riendeau D, Percival MD.

Protein Expr Purif. 2002 Dec;26(3):489-95.

PMID:
12460774
46.
47.

Thermodynamic analysis of the binding of aromatic hydroxamic acid analogues to ferric horseradish peroxidase.

Aitken SM, Turnbull JL, Percival MD, English AM.

Biochemistry. 2001 Nov 20;40(46):13980-9.

PMID:
11705389
48.

Mechanism of acetaminophen inhibition of cyclooxygenase isoforms.

Ouellet M, Percival MD.

Arch Biochem Biophys. 2001 Mar 15;387(2):273-80.

PMID:
11370851
49.

Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2.

Riendeau D, Percival MD, Brideau C, Charleson S, Dubé D, Ethier D, Falgueyret JP, Friesen RW, Gordon R, Greig G, Guay J, Mancini J, Ouellet M, Wong E, Xu L, Boyce S, Visco D, Girard Y, Prasit P, Zamboni R, Rodger IW, Gresser M, Ford-Hutchinson AW, Young RN, Chan CC.

J Pharmacol Exp Ther. 2001 Feb;296(2):558-66.

PMID:
11160644
50.

Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.

Falgueyret JP, Oballa RM, Okamoto O, Wesolowski G, Aubin Y, Rydzewski RM, Prasit P, Riendeau D, Rodan SB, Percival MD.

J Med Chem. 2001 Jan 4;44(1):94-104.

PMID:
11141092

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