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Items: 13

1.

Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.

Cheung M, Bao W, Behm DJ, Brooks CA, Bury MJ, Dowdell SE, Eidam HS, Fox RM, Goodman KB, Holt DA, Lee D, Roethke TJ, Willette RN, Xu X, Ye G, Thorneloe KS.

ACS Med Chem Lett. 2017 Mar 20;8(5):549-554. doi: 10.1021/acsmedchemlett.7b00094. eCollection 2017 May 11.

2.

An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.

Thorneloe KS, Cheung M, Bao W, Alsaid H, Lenhard S, Jian MY, Costell M, Maniscalco-Hauk K, Krawiec JA, Olzinski A, Gordon E, Lozinskaya I, Elefante L, Qin P, Matasic DS, James C, Tunstead J, Donovan B, Kallal L, Waszkiewicz A, Vaidya K, Davenport EA, Larkin J, Burgert M, Casillas LN, Marquis RW, Ye G, Eidam HS, Goodman KB, Toomey JR, Roethke TJ, Jucker BM, Schnackenberg CG, Townsley MI, Lepore JJ, Willette RN.

Sci Transl Med. 2012 Nov 7;4(159):159ra148. doi: 10.1126/scitranslmed.3004276.

3.

NADPH oxidase-dependent and -independent mechanisms of reported inhibitors of reactive oxygen generation.

Gatto GJ Jr, Ao Z, Kearse MG, Zhou M, Morales CR, Daniels E, Bradley BT, Goserud MT, Goodman KB, Douglas SA, Harpel MR, Johns DG.

J Enzyme Inhib Med Chem. 2013 Feb;28(1):95-104. doi: 10.3109/14756366.2011.636360. Epub 2011 Dec 3.

PMID:
22136506
4.

CCR2 receptor antagonists: optimization of biaryl sulfonamides to increase activity in whole blood.

Wang GZ, Haile PA, Daniel T, Belot B, Viet AQ, Goodman KB, Sha D, Dowdell SE, Varga N, Hong X, Chakravorty S, Webb C, Cornejo C, Olzinski A, Bernard R, Evans C, Emmons A, Briand J, Chung CW, Quek R, Lee D, Gough PJ, Sehon CA.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7291-4. doi: 10.1016/j.bmcl.2011.10.038. Epub 2011 Oct 19.

PMID:
22047688
5.

GSK1562590, a slowly dissociating urotensin-II receptor antagonist, exhibits prolonged pharmacodynamic activity ex vivo.

Behm DJ, Aiyar NV, Olzinski AR, McAtee JJ, Hilfiker MA, Dodson JW, Dowdell SE, Wang GZ, Goodman KB, Sehon CA, Harpel MR, Willette RN, Neeb MJ, Leach CA, Douglas SA.

Br J Pharmacol. 2010 Sep;161(1):207-28. doi: 10.1111/j.1476-5381.2010.00889.x.

6.

Pharmacological inhibition of C-C chemokine receptor 2 decreases macrophage infiltration in the aortic root of the human C-C chemokine receptor 2/apolipoprotein E-/- mouse: magnetic resonance imaging assessment.

Olzinski AR, Turner GH, Bernard RE, Karr H, Cornejo CA, Aravindhan K, Hoang B, Ringenberg MA, Qin P, Goodman KB, Willette RN, Macphee CH, Jucker BM, Sehon CA, Gough PJ.

Arterioscler Thromb Vasc Biol. 2010 Feb;30(2):253-9. doi: 10.1161/ATVBAHA.109.198812. Epub 2009 Dec 3. Erratum in: Arterioscler Thromb Vasc Biol. 2010 Sep;30(9):e170.

PMID:
19965779
7.

Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors.

Goodman KB, Bury MJ, Cheung M, Cichy-Knight MA, Dowdell SE, Dunn AK, Lee D, Lieby JA, Moore ML, Scherzer DA, Sha D, Suarez DP, Murphy DJ, Harpel MR, Manas ES, McNulty DE, Annan RS, Matico RE, Schwartz BK, Trill JJ, Sweitzer TD, Wang DY, Keller PM, Krawiec JA, Jaye MC.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):27-30. doi: 10.1016/j.bmcl.2008.11.033. Epub 2008 Nov 14.

PMID:
19058966
8.

Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases.

Sehon CA, Wang GZ, Viet AQ, Goodman KB, Dowdell SE, Elkins PA, Semus SF, Evans C, Jolivette LJ, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Wright LL, Smith GK, Behm DJ, Bentley R, Doe CP, Hu E, Lee D.

J Med Chem. 2008 Nov 13;51(21):6631-4. doi: 10.1021/jm8005096. Epub 2008 Oct 9.

PMID:
18842034
9.

Aminomethylpiperazines as selective urotensin antagonists.

Hilfiker MA, Zhang D, Dowdell SE, Goodman KB, McAtee JJ, Dodson JW, Viet AQ, Wang GZ, Sehon CA, Behm DJ, Wu Z, Carballo LH, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4470-3. doi: 10.1016/j.bmcl.2008.07.067. Epub 2008 Jul 20.

PMID:
18674898
10.

Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.

McAtee JJ, Dodson JW, Dowdell SE, Erhard K, Girard GR, Goodman KB, Hilfiker MA, Jin J, Sehon CA, Sha D, Shi D, Wang F, Wang GZ, Wang N, Wang Y, Viet AQ, Yuan CC, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9. doi: 10.1016/j.bmcl.2008.05.058. Epub 2008 May 20.

PMID:
18524591
11.

Development of potent and selective small-molecule human Urotensin-II antagonists.

McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3500-3. doi: 10.1016/j.bmcl.2008.05.027. Epub 2008 May 10.

PMID:
18502123
12.

Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors.

Goodman KB, Cui H, Dowdell SE, Gaitanopoulos DE, Ivy RL, Sehon CA, Stavenger RA, Wang GZ, Viet AQ, Xu W, Ye G, Semus SF, Evans C, Fries HE, Jolivette LJ, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Jung DK, Wright LL, Smith GK, Behm DJ, Bentley R, Doe CP, Hu E, Lee D.

J Med Chem. 2007 Jan 11;50(1):6-9.

PMID:
17201405
13.

Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.

Stavenger RA, Cui H, Dowdell SE, Franz RG, Gaitanopoulos DE, Goodman KB, Hilfiker MA, Ivy RL, Leber JD, Marino JP Jr, Oh HJ, Viet AQ, Xu W, Ye G, Zhang D, Zhao Y, Jolivette LJ, Head MS, Semus SF, Elkins PA, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Jung DK, Wright LL, Smith GK, Behm DJ, Doe CP, Bentley R, Chen ZX, Hu E, Lee D.

J Med Chem. 2007 Jan 11;50(1):2-5.

PMID:
17201404

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