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Items: 37

1.

Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.

Côté B, Burch JD, Asante-Appiah E, Bayly C, Bédard L, Blouin M, Campeau LC, Cauchon E, Chan M, Chefson A, Coulombe N, Cromlish W, Debnath S, Deschênes D, Dupont-Gaudet K, Falgueyret JP, Forget R, Gagné S, Gauvreau D, Girardin M, Guiral S, Langlois E, Li CS, Nguyen N, Papp R, Plamondon S, Roy A, Roy S, Seliniotakis R, St-Onge M, Ouellet S, Tawa P, Truchon JF, Vacca J, Wrona M, Yan Y, Ducharme Y.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):917-22. doi: 10.1016/j.bmcl.2013.12.070. Epub 2013 Dec 24.

PMID:
24412110
2.

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
3.

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
4.

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
5.

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
6.

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
7.

Basal activation of p70S6K results in adipose-specific insulin resistance in protein-tyrosine phosphatase 1B -/- mice.

Ruffolo SC, Forsell PK, Yuan X, Desmarais S, Himms-Hagen J, Cromlish W, Wong KK, Kennedy BP.

J Biol Chem. 2007 Oct 19;282(42):30423-33. Epub 2007 Jul 30.

8.

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
9.

PTP1B-dependent insulin receptor phosphorylation/residency in the endocytic recycling compartment of CHO-IR cells.

Cromlish WA, Tang M, Kyskan R, Tran L, Kennedy BP.

Biochem Pharmacol. 2006 Nov 15;72(10):1279-92. Epub 2006 Sep 7.

PMID:
16956584
10.

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
11.

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
12.

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
13.

The development of potent non-peptidic PTP-1B inhibitors.

Dufresne C, Roy P, Wang Z, Asante-Appiah E, Cromlish W, Boie Y, Forghani F, Desmarais S, Wang Q, Skorey K, Waddleton D, Ramachandran C, Kennedy BP, Xu L, Gordon R, Chan CC, Leblanc Y.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):1039-42.

PMID:
15013019
14.

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
15.

3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.

Black WC, Brideau C, Chan CC, Charleson S, Cromlish W, Gordon R, Grimm EL, Hughes G, Leger S, Li CS, Riendeau D, Thérien M, Wang Z, Xu LJ, Prasit P.

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1195-8.

PMID:
12643942
16.

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
17.

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
18.

Development and validation of an intact cell assay for protein tyrosine phosphatases using recombinant baculoviruses.

Cromlish WA, Payette P, Kennedy BP.

Biochem Pharmacol. 1999 Nov 15;58(10):1539-46.

PMID:
10535744
19.

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
20.

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
21.

Increased insulin sensitivity and obesity resistance in mice lacking the protein tyrosine phosphatase-1B gene.

Elchebly M, Payette P, Michaliszyn E, Cromlish W, Collins S, Loy AL, Normandin D, Cheng A, Himms-Hagen J, Chan CC, Ramachandran C, Gresser MJ, Tremblay ML, Kennedy BP.

Science. 1999 Mar 5;283(5407):1544-8.

22.
23.

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.

24.

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
25.

Selective inhibition of cyclooxygenase-1 and -2 using intact insect cell assays.

Cromlish WA, Kennedy BP.

Biochem Pharmacol. 1996 Dec 13;52(11):1777-85.

PMID:
8986141
26.

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
27.

Functional identification of the active-site nucleophile of the human 85-kDa cytosolic phospholipase A2.

Huang Z, Payette P, Abdullah K, Cromlish WA, Kennedy BP.

Biochemistry. 1996 Mar 26;35(12):3712-21.

PMID:
8619991
28.

A natural disruption of the secretory group II phospholipase A2 gene in inbred mouse strains.

Kennedy BP, Payette P, Mudgett J, Vadas P, Pruzanski W, Kwan M, Tang C, Rancourt DE, Cromlish WA.

J Biol Chem. 1995 Sep 22;270(38):22378-85.

29.

Purification of baculovirus-overexpressed cytosolic phospholipase A2 using a single-step affinity column chromatography.

Abdullah KM, Leger S, Perrier H, Cromlish WA, Kennedy B, Gresser M.

Protein Expr Purif. 1995 Jun;6(3):291-7.

PMID:
7663164
30.

Human cytosolic phospholipase A2 expressed in insect cells is extensively phosphorylated on Ser-505.

Abdullah K, Cromlish WA, Payette P, Laliberté F, Huang Z, Street I, Kennedy BP.

Biochim Biophys Acta. 1995 May 11;1244(1):157-64.

PMID:
7766652
31.

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
32.

High-level expression of active human cyclooxygenase-2 in insect cells.

Cromlish WA, Payette P, Culp SA, Ouellet M, Percival MD, Kennedy BP.

Arch Biochem Biophys. 1994 Oct;314(1):193-9.

PMID:
7944394
33.

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
34.

Cloning and expression of rat prostaglandin endoperoxide synthase (cyclooxygenase)-2 cDNA.

Kennedy BP, Chan CC, Culp SA, Cromlish WA.

Biochem Biophys Res Commun. 1993 Dec 15;197(2):494-500.

PMID:
7916614
35.

Transcriptionally active immediate-early protein of pseudorabies virus binds to specific sites on class II gene promoters.

Cromlish WA, Abmayr SM, Workman JL, Horikoshi M, Roeder RG.

J Virol. 1989 May;63(5):1869-76.

36.

Transcriptional regulation by the immediate early protein of pseudorabies virus during in vitro nucleosome assembly.

Workman JL, Abmayr SM, Cromlish WA, Roeder RG.

Cell. 1988 Oct 21;55(2):211-9.

PMID:
2844412
37.

Prolactin (PRL) receptor induction in cultured rat hepatocytes: dual regulation by PRL and growth hormone.

Barash I, Cromlish W, Posner BI.

Endocrinology. 1988 Mar;122(3):1151-8.

PMID:
3342748

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