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Items: 10


Pharmacologic modulation of RORγt translates to efficacy in preclinical and translational models of psoriasis and inflammatory arthritis.

Xue X, Soroosh P, De Leon-Tabaldo A, Luna-Roman R, Sablad M, Rozenkrants N, Yu J, Castro G, Banie H, Fung-Leung WP, Santamaria-Babi L, Schlueter T, Albers M, Leonard K, Budelsky AL, Fourie AM.

Sci Rep. 2016 Dec 1;6:37977. doi: 10.1038/srep37977.


Oxysterols are agonist ligands of RORγt and drive Th17 cell differentiation.

Soroosh P, Wu J, Xue X, Song J, Sutton SW, Sablad M, Yu J, Nelen MI, Liu X, Castro G, Luna R, Crawford S, Banie H, Dandridge RA, Deng X, Bittner A, Kuei C, Tootoonchi M, Rozenkrants N, Herman K, Gao J, Yang XV, Sachen K, Ngo K, Fung-Leung WP, Nguyen S, de Leon-Tabaldo A, Blevitt J, Zhang Y, Cummings MD, Rao T, Mani NS, Liu C, McKinnon M, Milla ME, Fourie AM, Sun S.

Proc Natl Acad Sci U S A. 2014 Aug 19;111(33):12163-8. doi: 10.1073/pnas.1322807111. Epub 2014 Aug 4.


Heteroaromatic-aminomethyl quinolones: potent and selective iNOS inhibitors.

Durón SG, Lindstrom A, Bonnefous C, Zhang H, Chen X, Symons KT, Sablad M, Rozenkrants N, Zhang Y, Wang L, Yazdani N, Shiau AK, Noble SA, Rix P, Rao TS, Hassig CA, Smith ND.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1237-41. doi: 10.1016/j.bmcl.2011.11.073. Epub 2011 Nov 25.


Pharmacological characterization of KLYP961, a dual inhibitor of inducible and neuronal nitric-oxide synthases.

Symons KT, Nguyen PM, Massari ME, Anzola JV, Staszewski LM, Wang L, Yazdani N, Dorow S, Muhammad J, Sablad M, Rozenkrants N, Bonefous C, Payne JE, Rix PJ, Shiau AK, Noble SA, Smith ND, Hassig CA, Zhang Y, Rao TS.

J Pharmacol Exp Ther. 2011 Feb;336(2):468-78. doi: 10.1124/jpet.110.172817. Epub 2010 Oct 29.


Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models.

Bonnefous C, Payne JE, Roppe J, Zhuang H, Chen X, Symons KT, Nguyen PM, Sablad M, Rozenkrants N, Zhang Y, Wang L, Severance D, Walsh JP, Yazdani N, Shiau AK, Noble SA, Rix P, Rao TS, Hassig CA, Smith ND.

J Med Chem. 2009 May 14;52(9):3047-62. doi: 10.1021/jm900173b.


KLYP956 is a non-imidazole-based orally active inhibitor of nitric-oxide synthase dimerization.

Symons KT, Massari ME, Nguyen PM, Lee TT, Roppe J, Bonnefous C, Payne JE, Smith ND, Noble SA, Sablad M, Rozenkrants N, Zhang Y, Rao TS, Shiau AK, Hassig CA.

Mol Pharmacol. 2009 Jul;76(1):153-62. doi: 10.1124/mol.109.055434. Epub 2009 Apr 13.


Inhibition of inducible nitric oxide synthase expression by a novel small molecule activator of the unfolded protein response.

Symons KT, Massari ME, Dozier SJ, Nguyen PM, Jenkins D, Herbert M, Gahman TC, Noble SA, Rozenkrants N, Zhang Y, Rao TS, Shiau AK, Hassig CA.

Curr Chem Genomics. 2008 Sep 27;2:1-9. doi: 10.2174/1875397300802010001.


Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.

Hu Y, Ma L, Wu M, Wong MS, Li B, Corral S, Yu Z, Nomanbhoy T, Alemayehu S, Fuller SR, Rosenblum JS, Rozenkrants N, Minimo LC, Ripka WC, Szardenings AK, Kozarich JW, Shreder KR.

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4239-42.


A new alpha-helical extension promotes RNA binding by the dsRBD of Rnt1p RNAse III.

Leulliot N, Quevillon-Cheruel S, Graille M, van Tilbeurgh H, Leeper TC, Godin KS, Edwards TE, Sigurdsson ST, Rozenkrants N, Nagel RJ, Ares M, Varani G.

EMBO J. 2004 Jul 7;23(13):2468-77. Epub 2004 Jun 10.

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