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Items: 16


Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1).

Filipski KJ, Sammons MF, Bhattacharya SK, Panteleev J, Brown JA, Loria PM, Boehm M, Smith AC, Shavnya A, Conn EL, Song K, Weng Y, Facemire C, Jüppner H, Clerin V.

ACS Med Chem Lett. 2018 Apr 12;9(5):440-445. doi: 10.1021/acsmedchemlett.8b00013. eCollection 2018 May 10.


Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis.

Menhaji-Klotz E, Hesp KD, Londregan AT, Kalgutkar AS, Piotrowski DW, Boehm M, Song K, Ryder T, Beaumont K, Jones RM, Atkinson K, Brown JA, Litchfield J, Xiao J, Canterbury DP, Burford K, Thuma BA, Limberakis C, Jiao W, Bagley SW, Agarwal S, Crowell D, Pazdziorko S, Ward J, Price DA, Clerin V.

J Med Chem. 2018 Apr 26;61(8):3685-3696. doi: 10.1021/acs.jmedchem.8b00190. Epub 2018 Apr 17.


Phosphodiesterase Type 5 Inhibition Reduces Albuminuria in Subjects with Overt Diabetic Nephropathy.

Scheele W, Diamond S, Gale J, Clerin V, Tamimi N, Le V, Walley R, Grover-Páez F, Perros-Huguet C, Rolph T, El Nahas M.

J Am Soc Nephrol. 2016 Nov;27(11):3459-3468. Epub 2016 Apr 25.


A zymogen-like factor Xa variant corrects the coagulation defect in hemophilia.

Ivanciu L, Toso R, Margaritis P, Pavani G, Kim H, Schlachterman A, Liu JH, Clerin V, Pittman DD, Rose-Miranda R, Shields KM, Erbe DV, Tobin JF, Arruda VR, Camire RM.

Nat Biotechnol. 2011 Oct 23;29(11):1028-33. doi: 10.1038/nbt.1995.


Discovery of 2-[1-(4-chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury.

Huang A, Moretto A, Janz K, Lowe M, Bedard PW, Tam S, Di L, Clerin V, Sushkova N, Tchernychev B, Tsao DH, Keith JC, Shaw GD, Schaub RG, Wang Q, Kaila N.

J Med Chem. 2010 Aug 26;53(16):6003-17. doi: 10.1021/jm9013696.


LXR ligand lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse.

Quinet EM, Basso MD, Halpern AR, Yates DW, Steffan RJ, Clerin V, Resmini C, Keith JC, Berrodin TJ, Feingold I, Zhong W, Hartman HB, Evans MJ, Gardell SJ, DiBlasio-Smith E, Mounts WM, LaVallie ER, Wrobel J, Nambi P, Vlasuk GP.

J Lipid Res. 2009 Dec;50(12):2358-70. doi: 10.1194/jlr.M900037-JLR200. Epub 2009 Mar 24.


Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.

Wrobel J, Steffan R, Bowen SM, Magolda R, Matelan E, Unwalla R, Basso M, Clerin V, Gardell SJ, Nambi P, Quinet E, Reminick JI, Vlasuk GP, Wang S, Feingold I, Huselton C, Bonn T, Farnegardh M, Hansson T, Nilsson AG, Wilhelmsson A, Zamaratski E, Evans MJ.

J Med Chem. 2008 Nov 27;51(22):7161-8. doi: 10.1021/jm800799q.


Expression of the cysteine protease legumain in vascular lesions and functional implications in atherogenesis.

Clerin V, Shih HH, Deng N, Hebert G, Resmini C, Shields KM, Feldman JL, Winkler A, Albert L, Maganti V, Wong A, Paulsen JE, Keith JC Jr, Vlasuk GP, Pittman DD.

Atherosclerosis. 2008 Nov;201(1):53-66. doi: 10.1016/j.atherosclerosis.2008.01.016. Epub 2008 Feb 21.


Characterization of the novel P-selectin inhibitor PSI-697 [2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h] quinoline-4-carboxylic acid] in vitro and in rodent models of vascular inflammation and thrombosis.

Bedard PW, Clerin V, Sushkova N, Tchernychev B, Antrilli T, Resmini C, Keith JC Jr, Hennan JK, Kaila N, Debernardo S, Janz K, Wang Q, Crandall DL, Schaub RG, Shaw GD, Carter LL.

J Pharmacol Exp Ther. 2008 Feb;324(2):497-506. Epub 2007 Nov 16.


Further modification on phenyl acetic acid based quinolines as liver X receptor modulators.

Hu B, Jetter J, Kaufman D, Singhaus R, Bernotas R, Unwalla R, Quinet E, Savio D, Halpern A, Basso M, Keith J, Clerin V, Chen L, Liu QY, Feingold I, Huselton C, Azam F, Goos-Nilsson A, Wilhelmsson A, Nambi P, Wrobel J.

Bioorg Med Chem. 2007 May 15;15(10):3321-33. Epub 2007 Mar 12.


2-(4-Chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[H]quinoline-4-carboxylic acid (PSI-697): identification of a clinical candidate from the quinoline salicylic acid series of P-selectin antagonists.

Kaila N, Janz K, Huang A, Moretto A, DeBernardo S, Bedard PW, Tam S, Clerin V, Keith JC Jr, Tsao DH, Sushkova N, Shaw GD, Camphausen RT, Schaub RG, Wang Q.

J Med Chem. 2007 Jan 11;50(1):40-64.


Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.

Hu B, Collini M, Unwalla R, Miller C, Singhaus R, Quinet E, Savio D, Halpern A, Basso M, Keith J, Clerin V, Chen L, Resmini C, Liu QY, Feingold I, Huselton C, Azam F, Farnegardh M, Enroth C, Bonn T, Goos-Nilsson A, Wilhelmsson A, Nambi P, Wrobel J.

J Med Chem. 2006 Oct 19;49(21):6151-4.


Tissue engineering of arteries by directed remodeling of intact arterial segments.

Clerin V, Nichol JW, Petko M, Myung RJ, Gaynor JW, Gooch KJ.

Tissue Eng. 2003 Jun;9(3):461-72.


Mechanical environment, donor age, and presence of endothelium interact to modulate porcine artery viability ex vivo.

Clerin V, Gusic RJ, O'Brien J, Kirshbom PM, Myung RJ, Gaynor JW, Gooch KJ.

Ann Biomed Eng. 2002;30(9):1117-27.


Structural changes in porcine bioprosthetic valves of a left ventricular assist system in human patients.

Moczar M, Houël R, Ginat M, Clérin V, Wheeldon D, Loisance D.

J Heart Valve Dis. 2000 Jan;9(1):88-95; discussion 95-6.


Pseudointima in inflow conduits of left ventricular assist devices.

Houel R, Moczar M, Clerin V, Loisance DY.

Ann Thorac Surg. 1999 Aug;68(2):717-23.


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