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1912 related items for PubMed ID: 19671883

  • 1. 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.
    J Pharmacol Exp Ther; 2009 Nov; 331(2):598-608. PubMed ID: 19671883
    [Abstract] [Full Text] [Related]

  • 2. Dynamics of {beta}-amyloid reductions in brain, cerebrospinal fluid, and plasma of {beta}-amyloid precursor protein transgenic mice treated with a {gamma}-secretase inhibitor.
    Barten DM, Guss VL, Corsa JA, Loo A, Hansel SB, Zheng M, Munoz B, Srinivasan K, Wang B, Robertson BJ, Polson CT, Wang J, Roberts SB, Hendrick JP, Anderson JJ, Loy JK, Denton R, Verdoorn TA, Smith DW, Felsenstein KM.
    J Pharmacol Exp Ther; 2005 Feb; 312(2):635-43. PubMed ID: 15452193
    [Abstract] [Full Text] [Related]

  • 3. Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases beta-cleavage of amyloid precursor protein and amyloid-beta production in vivo.
    Hussain I, Hawkins J, Harrison D, Hille C, Wayne G, Cutler L, Buck T, Walter D, Demont E, Howes C, Naylor A, Jeffrey P, Gonzalez MI, Dingwall C, Michel A, Redshaw S, Davis JB.
    J Neurochem; 2007 Feb; 100(3):802-9. PubMed ID: 17156133
    [Abstract] [Full Text] [Related]

  • 4. 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.
    J Med Chem; 2008 Dec 11; 51(23):7348-51. PubMed ID: 19012391
    [Abstract] [Full Text] [Related]

  • 5. Pharmacodynamics of selective inhibition of γ-secretase by avagacestat.
    Albright CF, Dockens RC, Meredith JE, Olson RE, Slemmon R, Lentz KA, Wang JS, Denton RR, Pilcher G, Rhyne PW, Raybon JJ, Barten DM, Burton C, Toyn JH, Sankaranarayanan S, Polson C, Guss V, White R, Simutis F, Sanderson T, Gillman KW, Starrett JE, Bronson J, Sverdlov O, Huang SP, Castaneda L, Feldman H, Coric V, Zaczek R, Macor JE, Houston J, Berman RM, Tong G.
    J Pharmacol Exp Ther; 2013 Mar 11; 344(3):686-95. PubMed ID: 23275065
    [Abstract] [Full Text] [Related]

  • 6. Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition.
    Abramowski D, Wiederhold KH, Furrer U, Jaton AL, Neuenschwander A, Runser MJ, Danner S, Reichwald J, Ammaturo D, Staab D, Stoeckli M, Rueeger H, Neumann U, Staufenbiel M.
    J Pharmacol Exp Ther; 2008 Nov 11; 327(2):411-24. PubMed ID: 18687920
    [Abstract] [Full Text] [Related]

  • 7. Proteolytic processing of the Alzheimer's disease amyloid precursor protein in brain and platelets.
    Evin G, Zhu A, Holsinger RM, Masters CL, Li QX.
    J Neurosci Res; 2003 Nov 01; 74(3):386-92. PubMed ID: 14598315
    [Abstract] [Full Text] [Related]

  • 8. Structural optimization of a CXCR2-directed antagonist that indirectly inhibits gamma-secretase and reduces Abeta.
    Bakshi P, Jin C, Broutin P, Berhane B, Reed J, Mullan M.
    Bioorg Med Chem; 2009 Dec 01; 17(23):8102-12. PubMed ID: 19853461
    [Abstract] [Full Text] [Related]

  • 9. Catalytic site-directed gamma-secretase complex inhibitors do not discriminate pharmacologically between Notch S3 and beta-APP cleavages.
    Lewis HD, Pérez Revuelta BI, Nadin A, Neduvelil JG, Harrison T, Pollack SJ, Shearman MS.
    Biochemistry; 2003 Jun 24; 42(24):7580-6. PubMed ID: 12809514
    [Abstract] [Full Text] [Related]

  • 10. Pharmacological evidences for DFK167-sensitive presenilin-independent gamma-secretase-like activity.
    Sevalle J, Ayral E, Hernandez JF, Martinez J, Checler F.
    J Neurochem; 2009 Jul 24; 110(1):275-83. PubMed ID: 19457123
    [Abstract] [Full Text] [Related]

  • 11. Reductions in beta-amyloid concentrations in vivo by the gamma-secretase inhibitors BMS-289948 and BMS-299897.
    Anderson JJ, Holtz G, Baskin PP, Turner M, Rowe B, Wang B, Kounnas MZ, Lamb BT, Barten D, Felsenstein K, McDonald I, Srinivasan K, Munoz B, Wagner SL.
    Biochem Pharmacol; 2005 Feb 15; 69(4):689-98. PubMed ID: 15670587
    [Abstract] [Full Text] [Related]

  • 12. Γ-secretase modulators do not induce Aβ-rebound and accumulation of β-C-terminal fragment.
    Li T, Huang Y, Jin S, Ye L, Rong N, Yang X, Ding Y, Cheng Z, Zhang J, Wan Z, Harrison DC, Hussain I, Hall A, Lee DH, Lau LF, Matsuoka Y.
    J Neurochem; 2012 Apr 15; 121(2):277-86. PubMed ID: 22035227
    [Abstract] [Full Text] [Related]

  • 13. Immunotherapy against APP beta-secretase cleavage site improves cognitive function and reduces neuroinflammation in Tg2576 mice without a significant effect on brain abeta levels.
    Rakover I, Arbel M, Solomon B.
    Neurodegener Dis; 2007 Apr 15; 4(5):392-402. PubMed ID: 17536186
    [Abstract] [Full Text] [Related]

  • 14. The novel beta-secretase inhibitor KMI-429 reduces amyloid beta peptide production in amyloid precursor protein transgenic and wild-type mice.
    Asai M, Hattori C, Iwata N, Saido TC, Sasagawa N, Szabó B, Hashimoto Y, Maruyama K, Tanuma S, Kiso Y, Ishiura S.
    J Neurochem; 2006 Jan 15; 96(2):533-40. PubMed ID: 16336629
    [Abstract] [Full Text] [Related]

  • 15. 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.
    Bioorg Med Chem; 2009 Jul 01; 17(13):4708-17. PubMed ID: 19443228
    [Abstract] [Full Text] [Related]

  • 16. Quantitative pharmacokinetic/pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors.
    Lu Y, Zhang L, Nolan CE, Becker SL, Atchison K, Robshaw AE, Pustilnik LR, Osgood SM, Miller EH, Stepan AF, Subramanyam C, Efremov I, Hallgren AJ, Riddell D.
    J Pharmacol Exp Ther; 2011 Dec 01; 339(3):922-34. PubMed ID: 21930801
    [Abstract] [Full Text] [Related]

  • 17. In vivo beta-secretase 1 inhibition leads to brain Abeta lowering and increased alpha-secretase processing of amyloid precursor protein without effect on neuregulin-1.
    Sankaranarayanan S, Price EA, Wu G, Crouthamel MC, Shi XP, Tugusheva K, Tyler KX, Kahana J, Ellis J, Jin L, Steele T, Stachel S, Coburn C, Simon AJ.
    J Pharmacol Exp Ther; 2008 Mar 01; 324(3):957-69. PubMed ID: 18156464
    [Abstract] [Full Text] [Related]

  • 18. Inhibition of Abeta production by NF-kappaB inhibitors.
    Paris D, Patel N, Quadros A, Linan M, Bakshi P, Ait-Ghezala G, Mullan M.
    Neurosci Lett; 2007 Mar 19; 415(1):11-6. PubMed ID: 17223266
    [Abstract] [Full Text] [Related]

  • 19. Apolipoprotein E modulates gamma-secretase cleavage of the amyloid precursor protein.
    Irizarry MC, Deng A, Lleo A, Berezovska O, Von Arnim CA, Martin-Rehrmann M, Manelli A, LaDu MJ, Hyman BT, Rebeck GW.
    J Neurochem; 2004 Sep 19; 90(5):1132-43. PubMed ID: 15312168
    [Abstract] [Full Text] [Related]

  • 20. CD147 is a regulatory subunit of the gamma-secretase complex in Alzheimer's disease amyloid beta-peptide production.
    Zhou S, Zhou H, Walian PJ, Jap BK.
    Proc Natl Acad Sci U S A; 2005 May 24; 102(21):7499-504. PubMed ID: 15890777
    [Abstract] [Full Text] [Related]


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