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Items: 20

1.

Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2).

Rowbottom MW, Bain G, Calderon I, Lasof T, Lonergan D, Lai A, Huang F, Darlington J, Prodanovich P, Santini AM, King CD, Goulet L, Shannon KE, Ma GL, Nguyen K, MacKenna DA, Evans JF, Hutchinson JH.

J Med Chem. 2017 May 25;60(10):4403-4423. doi: 10.1021/acs.jmedchem.7b00345. Epub 2017 May 15.

PMID:
28471663
2.

Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX.

Hutchinson JH, Rowbottom MW, Lonergan D, Darlington J, Prodanovich P, King CD, Evans JF, Bain G.

ACS Med Chem Lett. 2017 Mar 1;8(4):423-427. doi: 10.1021/acsmedchemlett.7b00014. eCollection 2017 Apr 13.

3.

Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis.

Bain G, Shannon KE, Huang F, Darlington J, Goulet L, Prodanovich P, Ma GL, Santini AM, Stein AJ, Lonergan D, King CD, Calderon I, Lai A, Hutchinson JH, Evans JF.

J Pharmacol Exp Ther. 2017 Jan;360(1):1-13. Epub 2016 Oct 17.

PMID:
27754931
4.

Structural Basis for Inhibition of Human Autotaxin by Four Potent Compounds with Distinct Modes of Binding.

Stein AJ, Bain G, Prodanovich P, Santini AM, Darlington J, Stelzer NM, Sidhu RS, Schaub J, Goulet L, Lonergan D, Calderon I, Evans JF, Hutchinson JH.

Mol Pharmacol. 2015 Dec;88(6):982-92. doi: 10.1124/mol.115.100404. Epub 2015 Sep 14.

PMID:
26371182
5.

5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.

Stock NS, Bain G, Zunic J, Li Y, Ziff J, Roppe J, Santini A, Darlington J, Prodanovich P, King CD, Baccei C, Lee C, Rong H, Chapman C, Broadhead A, Lorrain D, Correa L, Hutchinson JH, Evans JF, Prasit P.

J Med Chem. 2011 Dec 8;54(23):8013-29. doi: 10.1021/jm2008369. Epub 2011 Nov 7.

PMID:
22059882
6.

Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.

Scott JM, Baccei C, Bain G, Broadhead A, Evans JF, Fagan P, Hutchinson JH, King C, Lorrain DS, Lee C, Prasit P, Prodanovich P, Santini A, Stearns BA.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6608-12. doi: 10.1016/j.bmcl.2011.01.024. Epub 2011 Jan 11.

PMID:
21958540
7.

Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation.

Bain G, Lorrain DS, Stebbins KJ, Broadhead AR, Santini AM, Prodanovich P, Darlington J, King CD, Lee C, Baccei C, Stearns B, Troung Y, Hutchinson JH, Prasit P, Evans JF.

J Pharmacol Exp Ther. 2011 Jul;338(1):290-301. doi: 10.1124/jpet.111.180430. Epub 2011 Apr 12.

PMID:
21487069
8.

Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.

Stock N, Volkots D, Stebbins K, Broadhead A, Stearns B, Roppe J, Parr T, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King C, Lee C, Lorrain DS, Prodanovich P, Santini A, Evans JF, Hutchinson JH, Prasit P.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):1036-40. doi: 10.1016/j.bmcl.2010.12.016. Epub 2010 Dec 9.

PMID:
21211969
9.

A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model.

Swaney JS, Chapman C, Correa LD, Stebbins KJ, Bundey RA, Prodanovich PC, Fagan P, Baccei CS, Santini AM, Hutchinson JH, Seiders TJ, Parr TA, Prasit P, Evans JF, Lorrain DS.

Br J Pharmacol. 2010 Aug;160(7):1699-713. doi: 10.1111/j.1476-5381.2010.00828.x.

10.

5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.

Stock N, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King C, Lee C, Lorrain DS, Prodanovich P, Santini A, Schaab K, Evans JF, Hutchinson JH, Prasit P.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4598-601. doi: 10.1016/j.bmcl.2010.06.011. Epub 2010 Jun 8.

PMID:
20566292
11.

Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation.

Lorrain DS, Bain G, Correa LD, Chapman C, Broadhead AR, Santini AM, Prodanovich PP, Darlington JV, Stock NS, Zunic J, King CD, Lee C, Baccei CS, Stearns B, Roppe J, Hutchinson JH, Prasit P, Evans JF.

Eur J Pharmacol. 2010 Aug 25;640(1-3):211-8. doi: 10.1016/j.ejphar.2010.05.003. Epub 2010 May 21.

PMID:
20519143
12.

Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung.

Stebbins KJ, Broadhead AR, Baccei CS, Scott JM, Truong YP, Coate H, Stock NS, Santini AM, Fagan P, Prodanovich P, Bain G, Stearns BA, King CD, Hutchinson JH, Prasit P, Evans JF, Lorrain DS.

J Pharmacol Exp Ther. 2010 Mar;332(3):764-75. doi: 10.1124/jpet.109.161919. Epub 2009 Dec 8.

PMID:
19996299
13.

5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.

Stock N, Baccei C, Bain G, Broadhead A, Chapman C, Darlington J, King C, Lee C, Li Y, Lorrain DS, Prodanovich P, Rong H, Santini A, Zunic J, Evans JF, Hutchinson JH, Prasit P.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):213-7. doi: 10.1016/j.bmcl.2009.10.131. Epub 2009 Oct 31.

PMID:
19914828
14.

Pharmacological characterization of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103), a novel selective 5-lipoxygenase-activating protein inhibitor that reduces acute and chronic inflammation.

Lorrain DS, Bain G, Correa LD, Chapman C, Broadhead AR, Santini AM, Prodanovich P, Darlington JV, Hutchinson JH, King C, Lee C, Baccei C, Li Y, Arruda JM, Evans JF.

J Pharmacol Exp Ther. 2009 Dec;331(3):1042-50. doi: 10.1124/jpet.109.158089. Epub 2009 Sep 11.

PMID:
19749079
15.

5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).

Hutchinson JH, Li Y, Arruda JM, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King CD, Lee C, Lorrain D, Prodanovich P, Rong H, Santini A, Stock N, Prasit P, Evans JF.

J Med Chem. 2009 Oct 8;52(19):5803-15. doi: 10.1021/jm900945d.

PMID:
19739647
16.

Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.

Stearns BA, Baccei C, Bain G, Broadhead A, Clark RC, Coate H, Evans JF, Fagan P, Hutchinson JH, King C, Lee C, Lorrain DS, Prasit P, Prodanovich P, Santini A, Scott JM, Stock NS, Truong YP.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51. doi: 10.1016/j.bmcl.2009.06.085. Epub 2009 Jun 25.

PMID:
19608418
17.

Differential distribution of voltage-gated calcium channel alpha-2 delta (alpha2delta) subunit mRNA-containing cells in the rat central nervous system and the dorsal root ganglia.

Cole RL, Lechner SM, Williams ME, Prodanovich P, Bleicher L, Varney MA, Gu G.

J Comp Neurol. 2005 Oct 24;491(3):246-69.

PMID:
16134135
18.

Structure and functional characterization of a novel human low-voltage activated calcium channel.

Williams ME, Washburn MS, Hans M, Urrutia A, Brust PF, Prodanovich P, Harpold MM, Stauderman KA.

J Neurochem. 1999 Feb;72(2):791-9.

19.

Human immunodeficiency virus type 1 mutants resistant to nonnucleoside inhibitors of reverse transcriptase arise in tissue culture.

Richman D, Shih CK, Lowy I, Rose J, Prodanovich P, Goff S, Griffin J.

Proc Natl Acad Sci U S A. 1991 Dec 15;88(24):11241-5.

20.

Use of self-sustained sequence replication amplification reaction to analyze and detect mutations in zidovudine-resistant human immunodeficiency virus.

Gingeras TR, Prodanovich P, Latimer T, Guatelli JC, Richman DD, Barringer KJ.

J Infect Dis. 1991 Dec;164(6):1066-74.

PMID:
1955709

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