Identification of small molecule inhibitors of neurite loss induced by Aβ peptide using high content screening

Journal of Biological Chemistry

Volumn 287, Issue 12, 2012, Pages 8714-8723

  Ofengeim, Dimitry ^a   Shi, Peng ^b   Miao, Benchun ^c   Fan, Jing ^b   Xia, Ofeng ^b   Fan, Yubo ^b   Lipinski, Marta M ^a   Hashimoto, Tadafumi ^d   Polydoro, Manuela ^d   Yuan, Junying ^a   Wong, Stephen T C ^b   Degterev, Alexei ^c  

^a HARVARD MEDICAL SCHOOL   (United States)

^b HOUSTON METHODIST RESEARCH INSTITUTE   (United States)

^c TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^d MASSACHUSETTS GENERAL HOSPITAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVITY CLUSTERING; ALZHEIMER DISEASE; ANIMAL MODEL; BIOACTIVES; COGNITIVE FUNCTIONS; CYCLOOXYGENASE 2; DETRIMENTAL EFFECTS; DRUG DISCOVERY; HIGH-CONTENT SCREENING; MECHANISM OF ACTION; NEURITES; NEUROLOGICAL DISORDERS; NEUROPROTECTION; NON-STEROIDAL ANTI-INFLAMMATORY DRUGS; PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR; POTENTIAL DRUG; SMALL MOLECULE INHIBITOR; SMALL MOLECULES;

CYTOLOGY; DIAGNOSIS; MOLECULES; PEPTIDES;

NEURONS;

ACETYLSALICYLIC ACID; AMPROLIUM; AMYLOID BETA PROTEIN; ANTAZOLINE; AZAPERONE; BETA ESCIN; BUSULFAN; CEFOXITIN; CYCLOOXYGENASE 2; CYCLOPHOSPHAMIDE; ERYTHROMYCIN STEARATE; GAMBOGIC ACID; IBUPROFEN; IRINOTECAN; LIDOCAINE; MELOXICAM; METACETAMOL; MITOMYCIN C; NIMUSTINE; NONSTEROID ANTIINFLAMMATORY AGENT; NYSTATIN; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PROCAINE; PUROMYCIN; SULFADIAZINE; THIOTEPA; TRAZODONE; TRIMETHOPRIM; UNINDEXED DRUG; VANCOMYCIN;

ALZHEIMER DISEASE; ANIMAL CELL; ARTICLE; CELL LOSS; COMPUTER PROGRAM; CONTROLLED STUDY; DRUG ACTIVITY; DRUG IDENTIFICATION; DRUG MECHANISM; EMBRYO; HIGH CONTENT SCREENING; MOUSE; NERVE FIBER DEGENERATION; NEUROPROTECTION; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; SCREENING;

ALZHEIMER DISEASE; AMYLOID BETA-PEPTIDES; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; CYCLOOXYGENASE 2 INHIBITORS; DRUG EVALUATION, PRECLINICAL; HUMANS; NERVE DEGENERATION; NEURITES; PPAR GAMMA; SMALL MOLECULE LIBRARIES;

ANIMALIA;

EID: 84858598107     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M111.290957     Document Type: Article

References (30)

1. Palop, J. J., and Mucke, L. (2010) Amyloid-β-induced neuronal dysfunction in Alzheimer disease: from synapses toward neural networks. Nat. Neurosci. 13, 812-818
2. Knobloch, M., and Mansuy, I. M. (2008) Dendritic spine loss and synaptic alterations in Alzheimer disease. Mol. Neurobiol. 37, 73-82
3. Shankar, G. M., Li, S., Mehta, T. H., Garcia-Munoz, A., Shepardson, N. E., Smith, I., Brett, F. M., Farrell, M. A., Rowan, M. J., Lemere, C. A., Regan, C. M., Walsh, D. M., Sabatini, B. L., and Selkoe, D. J. (2008) Amyloid-β protein dimers isolated directly from Alzheimer's brains impair synaptic plasticity and memory. Nat. Med. 14, 837-842
4. Irizarry, M. C., McNamara, M., Fedorchak, K., Hsiao, K., and Hyman, B. T. (1997) APPSw transgenic mice develop age-related Aβ deposits and neuropil abnormalities, but no neuronal loss in CA1. J. Neuropathol. Exp. Neurol. 56, 965-973 (Pubitemid 27386126)
5. Schmidt, E. R., Pasterkamp, R. J., and van den Berg, L. H. (2009) Axon guidance proteins: novel therapeutic targets for ALS? Progress Neurobiol. 88, 286-301
6. Jellinger, K. A. (2009) Formation and development of Lewy pathology: a critical update. J. Neurol. 256, Suppl. 3, 270-279
7. Szekely, C. A., and Zandi, P. P. (2010) Non-steroidal anti-inflammatory drugs and Alzheimer disease: the epidemiological evidence. CNS Neurological Disorders Drug Targets 9, 132-139
8. Zhang, Y., Zhou, X., Degterev, A., Lipinski, M., Adjeroh, D., Yuan, J., and Wong, S. T. (2007) A novel tracing algorithm for high throughput imaging. Screening of neuron-based assays. J. Neurosci. Methods 160, 149-162 (Pubitemid 46137998)
9. Huang, Y., Zhou, X., Miao, B., Lipinski, M., Zhang, Y., Li, F., Degterev, A., Yuan, J., Hu, G., and Wong, S. T. (2010) A computational framework for studying neuron morphology from in vitro high content neuron-based screening. J. Neurosci. Methods 190, 299-309
10. Loh, S. H., Francescut, L., Lingor, P., Bähr, M., and Nicotera, P. (2008) Identification of new kinase clusters required for neurite outgrowth and retraction by a loss-of-function RNA interference screen. Cell Death Differ. 15, 283-298
11. Cole, G. M., and Frautschy, S. A. (2010) Mechanisms of action of nonsteroidal anti-inflammatory drugs for the prevention of Alzheimer disease. CNS Neurological Disorders Drug Targets 9, 140-148
12. Dargahi, L., Nasiraei-Moghadam, S., Abdi, A., Khalaj, L., Moradi, F., and Ahmadiani, A. (2011) Cyclooxygenase (COX)-1 activity precedes the COX-2 induction in Aβ-induced neuroinflammation. J. Mol. Neurosci. 45, 10-21
13. Jarrett, J. T., Berger, E. P., and Lansbury, P. T., Jr. (1993) The C-terminus of the beta protein is critical in amyloidogenesis. Ann. N.Y. Acad. Sci. 695, 144-148 (Pubitemid 23348252)
14. Dill, J., Patel, A. R., Yang, X. L., Bachoo, R., Powell, C. M., and Li, S. (2010) A molecular mechanism for ibuprofen-mediated RhoA inhibition in neurons. J. Neurosci. 30, 963-972
15. Selkoe, D. J. (2002) Deciphering the genesis and fate of amyloid beta-protein yields novel therapies for Alzheimer disease. J. Clinic. Investig. 110, 1375-1381
16. Sperling, R. A., Aisen, P. S., Beckett, L. A., Bennett, D. A., Craft, S., Fagan, A. M., Iwatsubo, T., Jack, C. R., Kaye, J., Montine, T. J., Park, D. C., Reiman, E. M., Rowe, C. C., Siemers, E., Stern, Y., Yaffe, K., Carrillo, M. C., Thies, B., Morrison-Bogorad, M., Wagster, M. V., and Phelps, C. H. (2011) Alzheimers Dement. 7, 280-292
17. Conejero-Goldberg, C. T., and Davies, P. (2008) Effects of cell cycle inhibitors on tau phosphorylation in N2aTau3R cells. J. Mol. Neurosci. 35, 7
18. Brioni, J. D., Garrison, T. R., Bitner, S. R., and Cowart, M. D. (2011) Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease. J. Pharmacol. Exp. Ther. 336, 13
19. Lee, Y. J., Han, S. B., Nam, S. Y., Oh, K. W., and Hong, J. T. (2010) Inflammation and Alzheimer disease. Arch. Pharm. Res. 33, 1539-1556
20. Kotilinek, L. A., Westerman, M. A., Wang, Q., Panizzon, K., Lim, G. P., Simonyi, A., Lesne, S., Falinska, A., Younkin, L. H., Younkin, S. G., Rowan, M., Cleary, J., Wallis, R. A., Sun, G. Y., Cole, G., Frautschy, S., Anwyl, R., and Ashe, K. H. (2008) Cyclooxygenase-2 inhibition improves amyloid-β-mediated suppression of memory and synaptic plasticity. Brain 131, 651-664 (Pubitemid 351294724)
21. Cakala, M., Malik, A. R., and Strosznajder, J. B. (2007) Inhibitor of cyclooxygenase-2 protects against amyloid β peptide-evoked memory impairment in mice. Pharmacol. Reports 59, 164-172 (Pubitemid 46957315)
22. Takeda, T., Kumar, R., Raman, E. P., and Klimov, D. K. (2010) Nonsteroidal anti-inflammatory drug naproxen destabilizes Aβ amyloid fibrils: a molecular dynamics investigation. J. Phys. Chem. B 114, 15394-15402
23. Fu, Q., Hue, J., and Li, S. (2007) Nonsteroidal anti-inflammatory drugs promote axon regeneration via RhoA inhibition. J Neurosci. 27, 4154-4164 (Pubitemid 46597154)
24. Weggen, S., Eriksen, J. L., Das, P., Sagi, S. A., Wang, R., Pietrzik, C. U., Findlay, K. A., Smith, T. E., Murphy, M. P., Bulter, T., Kang, D. E., Marquez-Sterling, N., Golde, T. E., and Koo, E. H. (2001) A subset of NSAIDs lower amyloidogenic Aβ42 independently of cyclooxygenase activity. Nature 414, 212-216 (Pubitemid 33051236)
25. Vlad, S. C., Miller, D. R., Kowall, N. W., and Felson, D. T. (2008) Protective effects of NSAIDs on the development of Alzheimer disease. Neurology 70, 1672-1677 (Pubitemid 351644133)
26. Hayden, K. M., Zandi, P. P., Khachaturian, A. S., Szekely, C. A., Fotuhi, M., Norton, M. C., Tschanz, J. T., Pieper, C. F., Corcoran, C., Lyketsos, C. G., Breitner, J. C., and Welsh-Bohmer, K. A. (2007) Does NSAID use modify cognitive trajectories in the elderly? The Cache County study. Neurology 69, 275-282 (Pubitemid 47205690)
27. Szekely, C. A., Breitner, J. C., Fitzpatrick, A. L., Rea, T. D., Psaty, B. M., Kuller, L. H., and Zandi, P. P. (2008) NSAID use and dementia risk in the Cardiovascular Health Study: role of APOE and NSAID type. Neurology 70, 17-24
28. Grodstein, F., Skarupski, K. A., Bienias, J. L., Wilson, R. S., Bennett, D. A., and Evans, D. A. (2008) Anti-inflammatory agents and cognitive decline in a bi-racial population. Neuroepidemiology 30, 45-50 (Pubitemid 351311725)
29. Aisen, P. S., Schafer, K. A., Grundman, M., Pfeiffer, E., Sano, M., Davis, K. L., Farlow, M. R., Jin, S., Thomas, R. G., and Thal, L. J. (2003) Effects of rofecoxib or naproxen vs placebo on Alzheimer disease progression: a randomized controlled trial. JAMA 289, 2819-2826 (Pubitemid 37430117)
30. Sato, T., Hanyu, H., Hirao, K., Kanetaka, H., Sakurai, H., and Iwamoto, T. (2011) Efficacy of PPAR-γ agonist pioglitazone in mild Alzheimer disease. Neurobiol. Aging 32, 1626-1633