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Hit-to-Lead Optimization and Discovery of 5-((5-([1,1'-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase.
Lan P, Romero FA, Wodka D, Kassick AJ, Dang Q, Gibson T, Cashion D, Zhou G, Chen Y, Zhang X, Zhang A, Li Y, Trujillo ME, Shao Q, Wu M, Xu S, He H, MacKenna D, Staunton J, Chapman KT, Weber A, Sebhat IK, Makara GM. Lan P, et al. Among authors: mackenna d. J Med Chem. 2017 Nov 9;60(21):9040-9052. doi: 10.1021/acs.jmedchem.7b01344. Epub 2017 Oct 25. J Med Chem. 2017. PMID: 29035567
A Potent and Selective AMPK Activator That Inhibits de Novo Lipogenesis.
Gómez-Galeno JE, Dang Q, Nguyen TH, Boyer SH, Grote MP, Sun Z, Chen M, Craigo WA, van Poelje PD, MacKenna DA, Cable EE, Rolzin PA, Finn PD, Chi B, Linemeyer DL, Hecker SJ, Erion MD. Gómez-Galeno JE, et al. Among authors: mackenna da. ACS Med Chem Lett. 2010 Aug 30;1(9):478-82. doi: 10.1021/ml100143q. eCollection 2010 Dec 9. ACS Med Chem Lett. 2010. PMID: 24900234 Free PMC article.
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. Rowbottom MW, et al. Among authors: mackenna da. J Med Chem. 2017 May 25;60(10):4403-4423. doi: 10.1021/acs.jmedchem.7b00345. Epub 2017 May 15. J Med Chem. 2017. PMID: 28471663
Lysyl oxidase like-2 contributes to renal fibrosis in Col4α3/Alport mice.
Cosgrove D, Dufek B, Meehan DT, Delimont D, Hartnett M, Samuelson G, Gratton MA, Phillips G, MacKenna DA, Bain G. Cosgrove D, et al. Among authors: mackenna da. Kidney Int. 2018 Aug;94(2):303-314. doi: 10.1016/j.kint.2018.02.024. Epub 2018 May 16. Kidney Int. 2018. PMID: 29759420 Free PMC article.
Liver-targeted drug delivery using HepDirect prodrugs.
Erion MD, van Poelje PD, Mackenna DA, Colby TJ, Montag AC, Fujitaki JM, Linemeyer DL, Bullough DA. Erion MD, et al. Among authors: mackenna da. J Pharmacol Exp Ther. 2005 Feb;312(2):554-60. doi: 10.1124/jpet.104.075903. Epub 2004 Aug 31. J Pharmacol Exp Ther. 2005. PMID: 15340017
Thyroid hormone beta receptor activation has additive cholesterol lowering activity in combination with atorvastatin in rabbits, dogs and monkeys.
Ito BR, Zhang BH, Cable EE, Song X, Fujitaki JM, MacKenna DA, Wilker CE, Chi B, van Poelje PD, Linemeyer DL, Erion MD. Ito BR, et al. Among authors: mackenna da. Br J Pharmacol. 2009 Feb;156(3):454-65. doi: 10.1111/j.1750-3639.2009.00038.x. Epub 2009 Jan 22. Br J Pharmacol. 2009. PMID: 19183199 Free PMC article.
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