Development of β-secretase Inhibitor as Drug for Alzheimerûs Disease

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Opa Vajragupta

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References

Asai M, Hattori C, Iwata N, et al. 2006. The novel beta-secretase inhibitor KMI-429 reduces amyloid beta peptide production in amyloid precursor protein transgenic and wild-type mice. J Neurochem 96 (2): 533-540.

Asberom T, Bara TA, Clader JW, et al. 2007. Tetra hydroquinoline sulfonamides as gamma- secretase inhibitors. Bioorg Med Chem Lett 17(1): 205-207.

Best JD, Jay MT, Otu F, Churcher I, et al. 2006. In vivo characterization of Abeta (40) changes in brain and cerebrospinal fluid usingn the novel gamma-secretaseinhibitor N-[cis-4-[(4- chlorophenyl) sulfonyl]-4-(2,5-difluoro- phenyl) cyclohexyl]-1,1, 1-trifluoromethane- sulfonamide (MRK-560) in the rat. J Pharmacol Exp Ther 317(2): 786-790.

Best JD, Jay MT, Otu F, et al. 2005. Quantitative measurement of changes in amyloid-beta (40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluoro- phenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl- 6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]- L-alaninamide]. J Pharmacol Exp Ther 313(2): 902-908.

Best JD, Smith DW, Reilly MA, et al. 2007. The novel gamma secretase inhibitor N-[cis-4-[(4- chlorophenyl) sulfonyl]-4-(2,5-difluoro phenyl) cyclohexyl]-1,1, 1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse. J Pharmacol Exp Ther 320(2): 552-558.

Citron M. 2004. Strategies for disease modification in Alzheimerûs disease. Nat Rev Neurosci 5(9):677-685.

Citron, M. 2002. Emerging Alzheimerûs disease therapies: inhibition of β-secretase. Neurobiol Aging 23(6): 1017-1022.

Fassa A, Parisiadou L, Robakis NK, et al. 2007. Novel processing of Notch 1 within its intracellular domain by a cysteine protease. Neurodegener Dis 4(2-3): 148-155.

Findeis, M. A. 2007. The role of amyloid beta peptide 42 in Alzheimerûs disease. Pharmacol Ther 116(2): 266-286.

Freskos JN, Fobian YM, Benson TE, et al. 2007a. Design of potent inhibitors of human beta-secretase. Part 1. Bioorg Med Chem Lett 17(1): 73-77.

Freskos JN, Fobian YM, Benson TE, et al. 2007b. Design of potent inhibitors of human beta-secretase. Part 2. Bioorg Med Chem Lett 17(1): 78-81.

Hamada Y, Igawa N, Ikari H, et al. 2006. Beta-Secretase inhibitors: Modification at the P4 position and improvement of inhibitory activity in cultured cells. Bioorg Med Chem Lett 16(16): 4354- 4359.

Higuchi M, Iwata N, Saido TC. 2005. Understanding molecular mechanisms of proteolysis in Alzheimerûs disease: Progress toward therapeutic interventions. Biochim Biophys Acta 1751(1): 60-67.

http://www.web-books.com/eLibrary/Medicine/Neurological/Alzheimer_Tau.htm

Hyde LA, McHugh NA, Chen J, et al. 2006. Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2- (3,5-difluorophenyl)-2-hydroxyethanoyl]-N1- [(7S)-5-methyl-6-oxo-6,7-dihydro-5H- dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY411,575) in the CRND8 mouse. J Pharmacol Exp Ther 319(3): 1133-1143.

Lindsley SR, Moore KP, Rajapakse HA, et al. 2007. Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors. Bioorg Med Chem Lett 17(14): 4057-4061.

Maillard MC, Hom RK, Benson TE, et al. 2007. Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase. J Med Chem 50(4): 776-781.

Mancini F, Naldi M, Cavrini V, et al. 2007. Multiwell fluorometric and colorimetric microassays for the evaluation of beta-secretase (BACE-1) inhibitors. Anal Bioanal Chem 388(5-6): 1175- 1183.

Mandel S, Weinreb O, Amit T, et al. 2005. Mechanism of neuroprotective action of the anti-Parkinson drug rasagiline and its derivatives. Brain Res Brain Res Rev 48(2): 379-387.

Pietrak BL, Crouthamel MC, Tugusheva K, et al. 2005. Biochemical and cell-based assays for characterization of BACE-1 inhibitors. Anal Biochem 342(1): 144-151.

Rajapakse HA, Nantermet PG, Selnick HG, 2006. D iscovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1). J Med Chem 49(25): 7270-7273.

Rojo I, Martin JA, Broughton H, et al. 2006. Macrocyclic peptidomimetic inhibitors of beta-secretase (BACE): first X-ray structure of a macrocyclic peptidomimetic-BACE complex. Bioorg Med Chem Lett 16(1): 191-195.

Takahashi Y, Fuwa H, Kaneko A, et al. 2006. Novel gamma-secretase inhibitors discovered by library screening of in-house synthetic natural product intermediates. Bioorg Med Chem Lett 16(14): 3813-3816.

Takeshita K, Satoh M, Ii M, et al. 2007. Critical role of endothelial Notch1 signaling in postnatal angiogenesis. Circ Res 100(1): 70-78.

Yeon SW, Jeon YJ, Hwang EM, et al. 2007. Effects of peptides derived from BACE1 catalytic domain on APP processing. Peptides 28(4): 838-844.