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Page 1
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.
Pu J, Kreft AF, Aschmies SH, Atchison KP, Berkowitz J, Caggiano TJ, Chlenov M, Diamantidis G, Harrison BL, Hu Y, Huryn D, Steven Jacobsen J, Jin M, Lipinski K, Lu P, Martone RL, Morris K, Sonnenberg-Reines J, Riddell DR, Sabalski J, Sun SC, Wagner E, Wang Y, Xu Z, Zhou H, Resnick L. Pu J, et al. Among authors: wagner e. Bioorg Med Chem. 2009 Jul 1;17(13):4708-17. doi: 10.1016/j.bmc.2009.04.052. Epub 2009 May 3. Bioorg Med Chem. 2009. PMID: 19443228
Acylguanidines as small-molecule beta-secretase inhibitors.
Cole DC, Manas ES, Stock JR, Condon JS, Jennings LD, Aulabaugh A, Chopra R, Cowling R, Ellingboe JW, Fan KY, Harrison BL, Hu Y, Jacobsen S, Jin G, Lin L, Lovering FE, Malamas MS, Stahl ML, Strand J, Sukhdeo MN, Svenson K, Turner MJ, Wagner E, Wu J, Zhou P, Bard J. Cole DC, et al. Among authors: wagner e. J Med Chem. 2006 Oct 19;49(21):6158-61. doi: 10.1021/jm0607451. J Med Chem. 2006. PMID: 17034121
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.
Jennings LD, Cole DC, Stock JR, Sukhdeo MN, Ellingboe JW, Cowling R, Jin G, Manas ES, Fan KY, Malamas MS, Harrison BL, Jacobsen S, Chopra R, Lohse PA, Moore WJ, O'Donnell MM, Hu Y, Robichaud AJ, Turner MJ, Wagner E, Bard J. Jennings LD, et al. Among authors: wagner e. Bioorg Med Chem Lett. 2008 Jan 15;18(2):767-71. doi: 10.1016/j.bmcl.2007.11.043. Epub 2007 Nov 17. Bioorg Med Chem Lett. 2008. PMID: 18068983
Discovery of a novel series of Notch-sparing gamma-secretase inhibitors.
Kreft A, Harrison B, Aschmies S, Atchison K, Casebier D, Cole DC, Diamantidis G, Ellingboe J, Hauze D, Hu Y, Huryn D, Jin M, Kubrak D, Lu P, Lundquist J, Mann C, Martone R, Moore W, Oganesian A, Porte A, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Woller K, Xu Z, Zhou H, Steven Jacobsen J. Kreft A, et al. Among authors: wagner e. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4232-6. doi: 10.1016/j.bmcl.2008.05.064. Epub 2008 May 20. Bioorg Med Chem Lett. 2008. PMID: 18556202
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Mayer SC, Kreft AF, Harrison B, Abou-Gharbia M, Antane M, Aschmies S, Atchison K, Chlenov M, Cole DC, Comery T, Diamantidis G, Ellingboe J, Fan K, Galante R, Gonzales C, Ho DM, Hoke ME, Hu Y, Huryn D, Jain U, Jin M, Kremer K, Kubrak D, Lin M, Lu P, Magolda R, Martone R, Moore W, Oganesian A, Pangalos MN, Porte A, Reinhart P, Resnick L, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Wang T, Woller K, Xu Z, Zaleska MM, Zeldis J, Zhang M, Zhou H, Jacobsen JS. Mayer SC, et al. Among authors: wagner e. J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w. J Med Chem. 2008. PMID: 19012391
(S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor.
Cole DC, Stock JR, Kreft AF, Antane M, Aschmies SH, Atchison KP, Casebier DS, Comery TA, Diamantidis G, Ellingboe JW, Harrison BL, Hu Y, Jin M, Kubrak DM, Lu P, Mann CW, Martone RL, Moore WJ, Oganesian A, Riddell DR, Sonnenberg-Reines J, Sun SC, Wagner E, Wang Z, Woller KR, Xu Z, Zhou H, Jacobsen JS. Cole DC, et al. Among authors: wagner e. Bioorg Med Chem Lett. 2009 Feb 1;19(3):926-9. doi: 10.1016/j.bmcl.2008.11.116. Epub 2008 Dec 6. Bioorg Med Chem Lett. 2009. PMID: 19097890
Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.
Martone RL, Zhou H, Atchison K, Comery T, Xu JZ, Huang X, Gong X, Jin M, Kreft A, Harrison B, Mayer SC, Aschmies S, Gonzales C, Zaleska MM, Riddell DR, Wagner E, Lu P, Sun SC, Sonnenberg-Reines J, Oganesian A, Adkins K, Leach MW, Clarke DW, Huryn D, Abou-Gharbia M, Magolda R, Bard J, Frick G, Raje S, Forlow SB, Balliet C, Burczynski ME, Reinhart PH, Wan HI, Pangalos MN, Jacobsen JS. Martone RL, et al. Among authors: wagner e. J Pharmacol Exp Ther. 2009 Nov;331(2):598-608. doi: 10.1124/jpet.109.152975. Epub 2009 Aug 11. J Pharmacol Exp Ther. 2009. PMID: 19671883
Enhanced clearance of Abeta in brain by sustaining the plasmin proteolysis cascade.
Jacobsen JS, Comery TA, Martone RL, Elokdah H, Crandall DL, Oganesian A, Aschmies S, Kirksey Y, Gonzales C, Xu J, Zhou H, Atchison K, Wagner E, Zaleska MM, Das I, Arias RL, Bard J, Riddell D, Gardell SJ, Abou-Gharbia M, Robichaud A, Magolda R, Vlasuk GP, Bjornsson T, Reinhart PH, Pangalos MN. Jacobsen JS, et al. Among authors: wagner e. Proc Natl Acad Sci U S A. 2008 Jun 24;105(25):8754-9. doi: 10.1073/pnas.0710823105. Epub 2008 Jun 16. Proc Natl Acad Sci U S A. 2008. PMID: 18559859 Free PMC article.
3,284 results