BACE-1 inhibition prevents the -secretase inhibitor evoked A rise in human neuroblastoma SH-SY5Y cells

Journal of Biomedical Science

Volumn 18, Issue 1, 2011, Pages

  Jämsä, Anne ^a   Belda, Oscar ^a   Edlund, Michael ^a   Lindström, Erik ^a  

^a MEDIVIR AB   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

AMYLOID BETA PROTEIN; AMYLOID BETA PROTEIN[1-40]; AMYLOID BETA PROTEIN[1-42]; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; GAMMA SECRETASE; N [1 BENZYL 3 (CYCLOPROPYLAMINO) 2 HYDROXYPROPYL] 7 ETHYL 1 METHYL 3,4 DIHYDRO 1H [1,2,5]THIADIAZEPINO[3,4,5 HI]INDOLE 9 CARBOXAMIDE 2,2 DIOXIDE; SEMAGACESTAT; UNCLASSIFIED DRUG; 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; ALANINE; AMYLOID BETA PROTEIN (1 42); AMYLOID BETA-PROTEIN (1-42); ASPARTIC PROTEINASE; AZEPINE DERIVATIVE; BACE1 PROTEIN, HUMAN; BENZOTHIADIAZINE DERIVATIVE; DRUG DERIVATIVE; N (1 BENZYL 3 (CYCLOPROPYLAMINO) 2 HYDROXYPROPYL) 7 ETHYL 1 METHYL 3,4 DIHYDRO 1H (1,2,5)THIADIAZEPINO(3,4,5 HI)INDOLE 9 CARBOXAMIDE 2,2 DIOXIDE; N-(1-BENZYL-3-(CYCLOPROPYLAMINO)-2-HYDROXYPROPYL)-7-ETHYL-1-METHYL-3,4-DIHYDRO-1H-(1,2,5)THIADIAZEPINO(3,4,5-HI)INDOLE-9-CARBOXAMIDE 2,2-DIOXIDE; 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; PEPTIDE FRAGMENT; SECRETASE; SULFOXIDE;

ARTICLE; CONTROLLED STUDY; DRUG EFFECT; DRUG MECHANISM; DRUG POTENTIATION; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; NEUROBLASTOMA CELL; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROTEIN SECRETION; ALZHEIMER DISEASE; DRUG ANTAGONISM; METABOLISM; TUMOR CELL LINE;

ALANINE; ALZHEIMER DISEASE; AMYLOID BETA-PEPTIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ASPARTIC ACID ENDOPEPTIDASES; AZEPINES; BENZOTHIADIAZINES; CELL LINE, TUMOR; CYCLIC S-OXIDES; HUMANS; PEPTIDE FRAGMENTS;

EID: 84857404716     PISSN: 10217770     EISSN: 14230127     Source Type: Journal    
DOI: 10.1186/1423-0127-18-76     Document Type: Article

References (23)

1. Amyloid precursor protein trafficking, processing and function. Thinkakaran G, Koo EH, J Biol Chem 2008 283 29615 29619 10.1074/jbc.R800019200 18650430
2. Amyloid-beta protein dimers isolated directly from Alzheimer's brains impair synaptic plasticity and memory. Shankar GM, Li S, Mehta TH, Garcia-Munoz A, Shepardson NE, Smith I, Brett FM, Farrell MA, Rowan MJ, Lemere CA, Regan CM, Walsh DM, Sabatini BL, Selkoe DJ, Nat Med 2008 14 837 842 10.1038/nm1782 18568035
3. A gamma-secretase inhibitor decreases amyloid-beta production in the central nervous system. Bateman RJ, Siemers ER, Mawuenyega KG, Wen G, Browning KR, Sigurdson WC, Yarasheski KE, Friedrich SW, Demattos RB, May PC, Paul SM, Holtzman DM, Ann Neurol 2009 66 1 48 54 10.1002/ana.21623 19360898
4. Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation. Wong GT, Manfra D, Poulet FM, Zhang Q, Josien H, Bara T, Engstrom L, Pinzon-Ortiz M, Fine JS, Lee HJ, Zhang L, Higgins GA, Parker EM, J Biol Chem 2004 279 12876 12882 14709552 (Pubitemid 38445862)
5. 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. Hyde LA, McHugh NA, Chen J, Zhang Q, Manfra D, Nomeir AA, Josien H, Bara T, Clader JW, Zhang L, Parker EM, Higgins GA, J Pharmacol Exp Ther 2006 319 1133 43 10.1124/jpet.106.111716 16946102
6. Development of semagacestat (LY450139), a functional -secretase inhibitor, for the treatment of Alzheimer's disease. Henley DB, May PC, Dean RA, Siemers ER, Expert Opin Pharmacother 2009 10 1657 1664 10.1517/ 14656560903044982 19527190
7. Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein -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 331 598 608 10.1124/jpet.109.152975 19671883
8. Recent advances in the identification of -secretase inhibitors to clinically test the A oligomer hypothesis of Alzheimer's Disease. Kreft AF, Martone R, Porte A, J Med Chem 2009 52 6169 6188 10.1021/jm900188z 19694467
9. Studies of Abeta pharmacodynamics in the brain, cerebrospinal fluid, and plasma in young (plaque-free) Tg2576 mice using 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 (LY-411575). Lanz TA, Hosley JD, Adams WJ, Merchant KM, J Pharmacol Exp Ther 2004 309 49 55 10.1124/jpet.103.060715 14718585 (Pubitemid 38393113)
10. Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139. Lanz TA, Karmilowicz MJ, Wood KM, Pozdnyakov N, Du P, Piotrowski MA, Brown TM, Nolan CE, Richter KEG, Finley JE, Fei Q, Ebbinghaus CF, Chen YL, Spracklin DK, Tate B, Geoghegan KF, Lau LF, Auperin DD, Schachter JB, J Pharmacol Exp Ther 2006 319 2 924 933 10.1124/jpet.106.110700 16920992
11. Safety, tolerability, and changes in amyloid beta concentrations after administration of a gamma-secretase inhibitor in volunteers. Siemers E, Skinner M, Dean RA, Gonzales C, Satterwhite J, Farlow M, Ness D, May PC, Clin Neuropharmacol 2005 28 3 126 32 10.1097/01.wnf.0000167360.27670.29 15965311 (Pubitemid 40923411)
12. The amyloid- rise and -secretase inhibitor potency depend on the level of substrate expression. Burton CR, Meredith JE, Barten DM, Goldstein ME, Krause CM, Kieras CJ, Sisk L, Iben LG, Polson C, Thompson MW, Lin XA, Corsa J, Fiedler T, Pierdomenico M, Cao Y, Roach AH, Cantone JL, Ford MJ, Drexler DM, Olson RE, Yang MG, Bergstrom CP, McElhone KE, Bronson JJ, Macor JE, Blat Y, Grafstrom RH, Stern AM, Sieffert DA, Zaczek R, Albright CF, Toyn JH, J Biol Chem 2008 283 22992 23003 10.1074/jbc.M804175200 18574238
13. Pharmacodynamics and pharmacokinetics of the -secretase inhibitor, PF-3084014. Lanz TA, Wood KM, Richter KEG, Nolan CE, Becker SL, Pozdnyakov N, Martin B-A, Du P, Oborski CE, Wood DE, Brown TM, Finley JE, Sokolowski SA, Hicks CD, Coffman KJ, Geoghegan KF, Brodney MA, Liston D, Tate B, J Pharmacol Exp Ther 2010 334 1 269 277 10.1124/jpet.110.167379 20363853
14. Lilly Halts Development of Semagacestat for Alzheimer's Disease Based on Preliminary Results of Phase III Clinical Trials. 2010 http://www.lilly.com
15. P-glycoprotein efflux and other factors limit brain amyloid reduction by -site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice. Meredith JE, Thompson LA, Toyn JH, Marcin L, Barten DM, Marcinkeviciene J, Kopcho L, Kim Y, Lin A, Guss V, Burton C, Iben L, Polson C, Cantone J, Ford M, Drexler D, Fiedler T, Lentz KA, Grace JE Jr, Kolb J, Corsa J, Pierdomenico M, Jones K, Olson RE, Macor JE, Albright CF, J Pharmacol Exp Ther 2008 326 502 513 10.1124/jpet.108.138974 18499745
16. In vivo inhibition of A production by memapsin 2 (-secretase) inhibitors. Chang W-P, Koelsch G, Wong S, Downs D, Da H, Weerasena V, Gordon B, Devasamudram T, Bilcer G, Ghosh AK, Tang J, J Neurochem 2004 89 1409 1416 10.1111/j.1471-4159.2004.02452.x 15189343 (Pubitemid 38802662)
17. Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases -cleavage of amyloid precursor protein and amyloid- 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 100 802 809 10.1111/j.1471-4159.2006.04260.x 17156133 (Pubitemid 46095629)
18. Macrocyclic peptidomimetic -secretase (BACE-1) inhibitors with activity in vivo. Machauer R, Laumen K, Veenstra S, Rondeau J-M, Tintelnot-Blomley M, Betsschart C, Jaton A-L, Desrayaud S, Staufenbiel M, Rabe S, Paganetti P, Neumann U, Bioorg Med Chem Lett 2009 19 1366 1370 10.1016/j.bmcl.2009.01.055 19195887
19. BACE1 inhibition reduces endogenous Abeta and alters APP processing in wild-type mice. Nishitomi K, Sakaguchi G, Horikoshi Y, Gray AJ, Maeda M, Hirata-Fukae C, Becker AG, Hosono M, Sakaguchi I, Minami SS, Nakajima Y, Li H-F, Takeyama C, Kihara T, Ota A, Wong PC, Aisen PS, Kato A, Kinoshita N, Matsuoka Y, J Neurochem 2006 99 1555 1563 10.1111/j.1471-4159.2006.04178.x 17083447 (Pubitemid 44924233)
20. First demonstration of cerebrospinal fluid and plasma A lowering with oral administration of a -site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates. Sankaranarayanan S, Holahan MA, Colussi D, Crouthamel M-C, Devanarayan V, Ellis J, Espeseth A, Gates AT, Graham SL, Gregro AR, Hazuda D, Hochman JH, Holloway K, Jin L, Kahana J, Lai M-T, Lineberger J, McGaughey G, Moore KP, Nantermet P, Pietrak B, Price EA, Rajapakse H, Stauffer S, Steinbeiser MA, Seabrook G, Selnick HG, Shi X-P, Stanton MG, Swestock J, Tugusheva K, Tyler KX, Vacca JP, Wong J, Wu G, Xu M, Cook JJ, Simon AJ, J Pharmacol Exp Ther 2009 328 131 140 10.1124/jpet.108.143628 18854490
21. US 2007/0299053. Audia JE, Diseroad BA, John V, Latimer LH, Nissen JS, Stephenson GA, Thorsett ED, Tung JS
22. Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability. Charrier N, Clarke B, Cutler L, Demont E, Dingwall C, Dunsdon R, East P, Hawkins J, Howes C, Hussain I, Jeffrey P, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redsahw S, Rowland P, Soleil V, Smith K, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G, J Med Chem 2008 51 11 3313 7 10.1021/jm800138h 18457381 (Pubitemid 351821890)
23. A pathogenic mutation for probable Alzheimer's disease in the APP gene at the N-terminus of beta-amyloid. Mullan M, Crawford F, Axelman K, Houlden H, Lilius L, Winblad B, Lannfelt L, Nat Genet 1992 1 345 347 10.1038/ng0892-345 1302033