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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: pangalos mn. 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
Early-onset behavioral and synaptic deficits in a mouse model of Alzheimer's disease.
Jacobsen JS, Wu CC, Redwine JM, Comery TA, Arias R, Bowlby M, Martone R, Morrison JH, Pangalos MN, Reinhart PH, Bloom FE. Jacobsen JS, et al. Among authors: pangalos mn. Proc Natl Acad Sci U S A. 2006 Mar 28;103(13):5161-6. doi: 10.1073/pnas.0600948103. Epub 2006 Mar 20. Proc Natl Acad Sci U S A. 2006. PMID: 16549764 Free PMC article.
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.
Zhou P, Li Y, Fan Y, Wang Z, Chopra R, Olland A, Hu Y, Magolda RL, Pangalos M, Reinhart PH, Turner MJ, Bard J, Malamas MS, Robichaud AJ. Zhou P, et al. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2326-9. doi: 10.1016/j.bmcl.2010.01.136. Epub 2010 Feb 12. Bioorg Med Chem Lett. 2010. PMID: 20202842
Design and synthesis of aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors with enhanced brain permeability.
Malamas MS, Robichaud A, Erdei J, Quagliato D, Solvibile W, Zhou P, Morris K, Turner J, Wagner E, Fan K, Olland A, Jacobsen S, Reinhart P, Riddell D, Pangalos M. Malamas MS, et al. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6597-605. doi: 10.1016/j.bmcl.2010.09.029. Epub 2010 Sep 15. Bioorg Med Chem Lett. 2010. PMID: 20880704
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: pangalos mn. 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.
Impact of apolipoprotein E (ApoE) polymorphism on brain ApoE levels.
Riddell DR, Zhou H, Atchison K, Warwick HK, Atkinson PJ, Jefferson J, Xu L, Aschmies S, Kirksey Y, Hu Y, Wagner E, Parratt A, Xu J, Li Z, Zaleska MM, Jacobsen JS, Pangalos MN, Reinhart PH. Riddell DR, et al. Among authors: pangalos mn. J Neurosci. 2008 Nov 5;28(45):11445-53. doi: 10.1523/JNEUROSCI.1972-08.2008. J Neurosci. 2008. PMID: 18987181 Free PMC article.
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: pangalos mn. J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w. J Med Chem. 2008. PMID: 19012391
156 results