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Discovery of a neuroprotective chemical, (S)-N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine [(-)-P7C3-S243], with improved druglike properties.
Naidoo J, De Jesus-Cortes H, Huntington P, Estill S, Morlock LK, Starwalt R, Mangano TJ, Williams NS, Pieper AA, Ready JM. Naidoo J, et al. Among authors: morlock lk. J Med Chem. 2014 May 8;57(9):3746-54. doi: 10.1021/jm401919s. Epub 2014 Apr 16. J Med Chem. 2014. PMID: 24697290 Free PMC article.
Development of proneurogenic, neuroprotective small molecules.
MacMillan KS, Naidoo J, Liang J, Melito L, Williams NS, Morlock L, Huntington PJ, Estill SJ, Longgood J, Becker GL, McKnight SL, Pieper AA, De Brabander JK, Ready JM. MacMillan KS, et al. J Am Chem Soc. 2011 Feb 9;133(5):1428-37. doi: 10.1021/ja108211m. Epub 2011 Jan 6. J Am Chem Soc. 2011. PMID: 21210688 Free PMC article.
A validated tumorgraft model reveals activity of dovitinib against renal cell carcinoma.
Sivanand S, Peña-Llopis S, Zhao H, Kucejova B, Spence P, Pavia-Jimenez A, Yamasaki T, McBride DJ, Gillen J, Wolff NC, Morlock L, Lotan Y, Raj GV, Sagalowsky A, Margulis V, Cadeddu JA, Ross MT, Bentley DR, Kabbani W, Xie XJ, Kapur P, Williams NS, Brugarolas J. Sivanand S, et al. Sci Transl Med. 2012 Jun 6;4(137):137ra75. doi: 10.1126/scitranslmed.3003643. Sci Transl Med. 2012. PMID: 22674553 Free PMC article.
Neuroprotective efficacy of aminopropyl carbazoles in a mouse model of amyotrophic lateral sclerosis.
Tesla R, Wolf HP, Xu P, Drawbridge J, Estill SJ, Huntington P, McDaniel L, Knobbe W, Burket A, Tran S, Starwalt R, Morlock L, Naidoo J, Williams NS, Ready JM, McKnight SL, Pieper AA. Tesla R, et al. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):17016-21. doi: 10.1073/pnas.1213960109. Epub 2012 Oct 1. Proc Natl Acad Sci U S A. 2012. PMID: 23027932 Free PMC article.
Neuroprotective efficacy of aminopropyl carbazoles in a mouse model of Parkinson disease.
De Jesús-Cortés H, Xu P, Drawbridge J, Estill SJ, Huntington P, Tran S, Britt J, Tesla R, Morlock L, Naidoo J, Melito LM, Wang G, Williams NS, Ready JM, McKnight SL, Pieper AA. De Jesús-Cortés H, et al. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):17010-5. doi: 10.1073/pnas.1213956109. Epub 2012 Oct 1. Proc Natl Acad Sci U S A. 2012. PMID: 23027934 Free PMC article.
Structure-based design and mechanisms of allosteric inhibitors for mitochondrial branched-chain α-ketoacid dehydrogenase kinase.
Tso SC, Qi X, Gui WJ, Chuang JL, Morlock LK, Wallace AL, Ahmed K, Laxman S, Campeau PM, Lee BH, Hutson SM, Tu BP, Williams NS, Tambar UK, Wynn RM, Chuang DT. Tso SC, et al. Among authors: morlock lk. Proc Natl Acad Sci U S A. 2013 Jun 11;110(24):9728-33. doi: 10.1073/pnas.1303220110. Epub 2013 May 28. Proc Natl Acad Sci U S A. 2013. PMID: 23716694 Free PMC article.
The P7C3 class of neuroprotective compounds exerts antidepressant efficacy in mice by increasing hippocampal neurogenesis.
Walker AK, Rivera PD, Wang Q, Chuang JC, Tran S, Osborne-Lawrence S, Estill SJ, Starwalt R, Huntington P, Morlock L, Naidoo J, Williams NS, Ready JM, Eisch AJ, Pieper AA, Zigman JM. Walker AK, et al. Mol Psychiatry. 2015 Apr;20(4):500-8. doi: 10.1038/mp.2014.34. Epub 2014 Apr 22. Mol Psychiatry. 2015. PMID: 24751964 Free PMC article.
Early detection of subclinical visual damage after blast-mediated TBI enables prevention of chronic visual deficit by treatment with P7C3-S243.
Dutca LM, Stasheff SF, Hedberg-Buenz A, Rudd DS, Batra N, Blodi FR, Yorek MS, Yin T, Shankar M, Herlein JA, Naidoo J, Morlock L, Williams N, Kardon RH, Anderson MG, Pieper AA, Harper MM. Dutca LM, et al. Invest Ophthalmol Vis Sci. 2014 Dec 2;55(12):8330-41. doi: 10.1167/iovs.14-15468. Invest Ophthalmol Vis Sci. 2014. PMID: 25468886 Free PMC article.
23 results