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1-(3',4'-Dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a novel gamma-secretase modulator, reduces brain beta-amyloid pathology in a transgenic mouse model of Alzheimer's disease without causing peripheral toxicity.
Imbimbo BP, Del Giudice E, Colavito D, D'Arrigo A, Dalle Carbonare M, Villetti G, Facchinetti F, Volta R, Pietrini V, Baroc MF, Serneels L, De Strooper B, Leon A. Imbimbo BP, et al. Among authors: serneels l. J Pharmacol Exp Ther. 2007 Dec;323(3):822-30. doi: 10.1124/jpet.107.129007. Epub 2007 Sep 25. J Pharmacol Exp Ther. 2007. PMID: 17895400
Differential contribution of the three Aph1 genes to gamma-secretase activity in vivo.
Serneels L, Dejaegere T, Craessaerts K, Horré K, Jorissen E, Tousseyn T, Hébert S, Coolen M, Martens G, Zwijsen A, Annaert W, Hartmann D, De Strooper B. Serneels L, et al. Proc Natl Acad Sci U S A. 2005 Feb 1;102(5):1719-24. doi: 10.1073/pnas.0408901102. Epub 2005 Jan 21. Proc Natl Acad Sci U S A. 2005. PMID: 15665098 Free PMC article.
ADAM10, the rate-limiting protease of regulated intramembrane proteolysis of Notch and other proteins, is processed by ADAMS-9, ADAMS-15, and the gamma-secretase.
Tousseyn T, Thathiah A, Jorissen E, Raemaekers T, Konietzko U, Reiss K, Maes E, Snellinx A, Serneels L, Nyabi O, Annaert W, Saftig P, Hartmann D, De Strooper B. Tousseyn T, et al. Among authors: serneels l. J Biol Chem. 2009 Apr 24;284(17):11738-47. doi: 10.1074/jbc.M805894200. Epub 2009 Feb 11. J Biol Chem. 2009. PMID: 19213735 Free PMC article.
65 results