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Page 1
Discovery and characterization of an inhibitor of glucosylceramide synthase.
Richards S, Larson CJ, Koltun ES, Hanel A, Chan V, Nachtigall J, Harrison A, Aay N, Du H, Arcalas A, Galan A, Zhang J, Zhang W, Won KA, Tam D, Qian F, Wang T, Finn P, Ogilvie K, Rosen J, Aoyama R, Plonowski A, Cancilla B, Bentzien F, Yakes M, Mohan R, Lamb P, Nuss J, Kearney P. Richards S, et al. Among authors: larson cj. J Med Chem. 2012 May 10;55(9):4322-35. doi: 10.1021/jm300122u. Epub 2012 Apr 19. J Med Chem. 2012. PMID: 22497444
Discovery of a new class of glucosylceramide synthase inhibitors.
Koltun E, Richards S, Chan V, Nachtigall J, Du H, Noson K, Galan A, Aay N, Hanel A, Harrison A, Zhang J, Won KA, Tam D, Qian F, Wang T, Finn P, Ogilvie K, Rosen J, Mohan R, Larson C, Lamb P, Nuss J, Kearney P. Koltun E, et al. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6773-7. doi: 10.1016/j.bmcl.2011.09.037. Epub 2011 Sep 17. Bioorg Med Chem Lett. 2011. PMID: 21974949
Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design-Part 1.
Cheruvallath Z, Tang M, McBride C, Komandla M, Miura J, Ton-Nu T, Erikson P, Feng J, Farrell P, Lawson JD, Vanderpool D, Wu Y, Dougan DR, Plonowski A, Holub C, Larson C. Cheruvallath Z, et al. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2774-2778. doi: 10.1016/j.bmcl.2016.04.073. Epub 2016 Apr 25. Bioorg Med Chem Lett. 2016. PMID: 27155900
Time-dependent inhibition of PHD2.
Tcholakov I, Grimshaw CE, Shi L, Kiryanov A, Murphy ST, Larson CJ, Plonowski A, Ermolieff J. Tcholakov I, et al. Among authors: larson cj. Biosci Rep. 2017 Jun 30;37(3):BSR20170275. doi: 10.1042/BSR20170275. Print 2017 Jun 30. Biosci Rep. 2017. PMID: 28592559 Free PMC article.
Chronic fractalkine administration improves glucose tolerance and pancreatic endocrine function.
Riopel M, Seo JB, Bandyopadhyay GK, Li P, Wollam J, Chung H, Jung SR, Murphy A, Wilson M, de Jong R, Patel S, Balakrishna D, Bilakovics J, Fanjul A, Plonowski A, Koh DS, Larson CJ, Olefsky JM, Lee YS. Riopel M, et al. Among authors: larson cj. J Clin Invest. 2018 Apr 2;128(4):1458-1470. doi: 10.1172/JCI94330. Epub 2018 Mar 5. J Clin Invest. 2018. PMID: 29504946 Free PMC article.
Using Target Engagement Biomarkers to Predict Clinical Efficacy of MetAP2 Inhibitors.
Farrell PJ, Zopf CJ, Huang HJ, Balakrishna D, Holub C, Bilakovics J, Fanjul A, Matuszkiewicz J, Plonowski A, Rolzin P, Banerjee U, Ermolieff J, Cheruvallath ZS, McBride C, Bartkowski D, Mazur C, Pachori A, Larson CJ. Farrell PJ, et al. Among authors: larson cj. J Pharmacol Exp Ther. 2019 Nov;371(2):299-308. doi: 10.1124/jpet.119.259028. Epub 2019 Sep 19. J Pharmacol Exp Ther. 2019. PMID: 31537613
Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site.
Montalban AG, Boman E, Chang CD, Ceide SC, Dahl R, Dalesandro D, Delaet NG, Erb E, Ernst JT, Gibbs A, Kahl J, Kessler L, Kucharski J, Lum C, Lundström J, Miller S, Nakanishi H, Roberts E, Saiah E, Sullivan R, Urban J, Wang Z, Larson CJ. Montalban AG, et al. Among authors: larson cj. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4819-24. doi: 10.1016/j.bmcl.2010.06.102. Bioorg Med Chem Lett. 2010. PMID: 20663667
The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.
Montalban AG, Boman E, Chang CD, Ceide SC, Dahl R, Dalesandro D, Delaet NG, Erb E, Ernst JT, Gibbs A, Kahl J, Kessler L, Lundström J, Miller S, Nakanishi H, Roberts E, Saiah E, Sullivan R, Wang Z, Larson CJ. Montalban AG, et al. Among authors: larson cj. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1772-7. doi: 10.1016/j.bmcl.2008.02.033. Epub 2008 Feb 16. Bioorg Med Chem Lett. 2008. PMID: 18325768
54 results