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Page 1
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.
Shen HC, Szymonifka MJ, Kharbanda D, Deng Q, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Taggart AK, Wang J, Tong X, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: wu kk, wu tj. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6723-8. doi: 10.1016/j.bmcl.2007.10.055. Epub 2007 Oct 18. Bioorg Med Chem Lett. 2007. PMID: 18029181
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.
Shen HC, Ding FX, Luell S, Forrest MJ, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Wilsie LC, Krsmanovic ML, Taggart AK, Ren N, Cai TQ, Deng Q, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: wu kk, wu tj. J Med Chem. 2007 Dec 13;50(25):6303-6. doi: 10.1021/jm700942d. Epub 2007 Nov 10. J Med Chem. 2007. PMID: 17994679
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
Shen HC, Ding FX, Deng Q, Wilsie LC, Krsmanovic ML, Taggart AK, Carballo-Jane E, Ren N, Cai TQ, Wu TJ, Wu KK, Cheng K, Chen Q, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: wu kk, wu tj. J Med Chem. 2009 Apr 23;52(8):2587-602. doi: 10.1021/jm900151e. J Med Chem. 2009. PMID: 19309152
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
Shen HC, Ding FX, Raghavan S, Deng Q, Luell S, Forrest MJ, Carballo-Jane E, Wilsie LC, Krsmanovic ML, Taggart AK, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL. Shen HC, et al. Among authors: wu kk, wu tj. J Med Chem. 2010 Mar 25;53(6):2666-70. doi: 10.1021/jm100022r. J Med Chem. 2010. PMID: 20184326
Niacin lipid efficacy is independent of both the niacin receptor GPR109A and free fatty acid suppression.
Lauring B, Taggart AK, Tata JR, Dunbar R, Caro L, Cheng K, Chin J, Colletti SL, Cote J, Khalilieh S, Liu J, Luo WL, Maclean AA, Peterson LB, Polis AB, Sirah W, Wu TJ, Liu X, Jin L, Wu K, Boatman PD, Semple G, Behan DP, Connolly DT, Lai E, Wagner JA, Wright SD, Cuffie C, Mitchel YB, Rader DJ, Paolini JF, Waters MG, Plump A. Lauring B, et al. Sci Transl Med. 2012 Aug 22;4(148):148ra115. doi: 10.1126/scitranslmed.3003877. Sci Transl Med. 2012. PMID: 22914621 Clinical Trial.
11beta-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice.
Hermanowski-Vosatka A, Balkovec JM, Cheng K, Chen HY, Hernandez M, Koo GC, Le Grand CB, Li Z, Metzger JM, Mundt SS, Noonan H, Nunes CN, Olson SH, Pikounis B, Ren N, Robertson N, Schaeffer JM, Shah K, Springer MS, Strack AM, Strowski M, Wu K, Wu T, Xiao J, Zhang BB, Wright SD, Thieringer R. Hermanowski-Vosatka A, et al. J Exp Med. 2005 Aug 15;202(4):517-27. doi: 10.1084/jem.20050119. J Exp Med. 2005. PMID: 16103409 Free PMC article.
11β-HSD1 inhibition reduces atherosclerosis in mice by altering proinflammatory gene expression in the vasculature.
Luo MJ, Thieringer R, Springer MS, Wright SD, Hermanowski-Vosatka A, Plump A, Balkovec JM, Cheng K, Ding GJ, Kawka DW, Koo GC, Grand CB, Luo Q, Maletic MM, Malkowitz L, Shah K, Singer I, Waddell ST, Wu KK, Yuan J, Zhu J, Stepaniants S, Yang X, Lum PY, Wang IM. Luo MJ, et al. Among authors: wu kk. Physiol Genomics. 2013 Jan 7;45(1):47-57. doi: 10.1152/physiolgenomics.00109.2012. Epub 2012 Nov 20. Physiol Genomics. 2013. PMID: 23170035
533 results