Identification of small molecule inhibitors of β-amyloid cytotoxicity through a cell-based high-throughput screening platform

Journal of Biomolecular Screening

Volumn 13, Issue 9, 2008, Pages 870-878

  Seyb, K I ^a,b,c   Schuman, E R ^b   Ni, J ^b   Huang, M M ^b   Michaelis, M L ^b   Glicksman, M A ^b  

^a UNIVERSITY OF KANSAS   (United States)

^b BRIGHAM AND WOMEN S HOSPITAL   (United States)

^c Laboratory for Drug Discovery in Neurodegeneration   (United States)

Author keywords

amyloid; Alzheimer's disease; Calpain; High throughput screen; Neurodegeneration

Indexed keywords

[1 [(1 FORMYL 2 PHENYLETHYL)CARBAMOYL] 2 METHYLPROPYL]CARBAMIC ACID BENZYL ESTER; AMYLOID BETA PROTEIN; CALPAIN; N ACETYLLEUCYLLEUCYLNORLEUCINAL; PROTEIN INHIBITOR;

ARTICLE; CELL ASSAY; CELL DEATH; CELL DIFFERENTIATION; CONTROLLED STUDY; CYTOTOXICITY; DRUG IDENTIFICATION; ENZYME ACTIVATION; ENZYME ACTIVITY; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC 50; NEUROPROTECTION; PRIORITY JOURNAL;

ALZHEIMER DISEASE; AMYLOID BETA-PROTEIN; CALCIUM; CALPAIN; CELL DEATH; CELL LINE, TUMOR; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; EGTAZIC ACID; HUMANS; LUMINESCENCE; MASS SCREENING; NEURODEGENERATIVE DISEASES; TIME FACTORS;

EID: 53649103225     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057108323909     Document Type: Article

References (27)

1. Yankner BA, Dawes LR, Fisher S., Villa-Komaroff L., Oster-Granite ML, Neve RL: Neurotoxicity of a fragment of the amyloid precursor associated with Alzheimer's disease. Science 1989 ; 245: 417-420.
2. Pike CJ, Walencewicz AJ, Glabe CG, Cotman CW: In vitro aging of beta-amyloid protein causes peptide aggregation and neurotoxicity. Brain Res 1991 ; 563: 311-314.
3. Yankner BA: Mechanisms of neuronal degeneration in Alzheimer's disease. Neuron 1996 ; 16: 921-932.
4. Feinstein SC, Wilson L.: Inability of tau to properly regulate neuronal microtubule dynamics: a loss-of-function mechanism by which tau might mediate neuronal cell death. Biochim Biophys Acta 2005 ; 1739: 268-279.
5. Alvarez A., Toro R., Caceres A., Maccioni RB: Inhibition of tau phosphorylating protein kinase cdk5 prevents beta-amyloid-induced neuronal death. FEBS Lett 1999 ; 459: 421-426.
6. Li G., Faibushevich A., Turunen BJ, Yoon SO, Georg G., Michaelis ML, Dobrowsky RT: Stabilization of the cyclin-dependent kinase 5 activator, p35, by paclitaxel decreases beta-amyloid toxicity in cortical neurons. J Neurochem 2003 ; 84: 347-362.
7. Lee KY, Clark AW, Rosales JL, Chapman K., Fung T., Johnston RN: Elevated neuronal Cdc2-like kinase activity in the Alzheimer disease brain. Neurosci Res 1999 ; 34: 21-29.
8. Patrick GN, Zukerberg L., Nikolic M., de la Monte S., Dikkes P., Tsai LH: Conversion of p35 to p25 deregulates Cdk5 activity and promotes neurodegeneration. Nature 1999 ; 402: 615-622.
9. Tsai LH, Delalle I., Caviness VS Jr, Chae T., Harlow E.: p35 is a neural-specific regulatory subunit of cyclin-dependent kinase 5. Nature 1994 ; 371: 419-423.
10. Humbert S., Dhavan R., Tsai L.: p39 activates cdk5 in neurons, and is associated with the actin cytoskeleton. J Cell Sci 2000 ; 113 (pt 6). 975-983.
11. Kusakawa G., Saito T., Onuki R., Ishiguro K., Kishimoto T., Hisanaga S.: Calpain-dependent proteolytic cleavage of the p35 cyclin-dependent kinase 5 activator to p25. J Biol Chem 2000 ; 275: 17166-17172.
12. Lee MS, Kwon YT, Li M., Peng J., Friedlander RM, Tsai LH: Neurotoxicity induces cleavage of p35 to p25 by calpain. Nature 2000 ; 405: 360-364.
13. Mattson MP, Cheng B., Davis D., Bryant K., Lieberburg I., Rydel RE: beta-Amyloid peptides destabilize calcium homeostasis and render human cortical neurons vulnerable to excitotoxicity. J Neurosci 1992 ; 12: 376-389.
14. He LM, Chen LY, Lou XL, Qu AL, Zhou Z., Xu T.: Evaluation of beta-amyloid peptide 25-35 on calcium homeostasis in cultured rat dorsal root ganglion neurons. Brain Res 2002 ; 939: 65-75.
15. Saito K., Elce JS, Hamos JE, Nixon RA: Widespread activation of calcium-activated neutral proteinase (calpain) in the brain in Alzheimer disease: a potential molecular basis for neuronal degeneration. Proc Natl Acad Sci U S A 1993 ; 90: 2628-2632.
16. Taniguchi S., Fujita Y., Hayashi S., Kakita A., Takahashi H., Murayama S.,, et al. Calpain-mediated degradation of p35 to p25 in postmortem human and rat brains. FEBS Lett 2001 ; 489: 46-50.
17. Siman R., Card JP, Davis LG: Proteolytic processing of beta-amyloid precursor by calpain I. J Neurosci 1990 ; 10: 2400-2411.
18. Chen M., Durr J., Fernandez HL: Possible role of calpain in normal processing of beta-amyloid precursor protein in human platelets. Biochem Biophys Res Commun 2000 ; 273: 170-175.
19. Kelly BL, Vassar R., Ferreira A.: Beta-amyloid-induced dynamin 1 depletion in hippocampal neurons: a potential mechanism for early cognitive decline in Alzheimer disease. J Biol Chem 2005 ; 280: 31746-31753.
20. Nakagawa T., Yuan J.: Cross-talk between two cysteine protease families: activation of caspase-12 by calpain in apoptosis. J Cell Biol 2000 ; 150: 887-894.
21. Schumacher PA, Siman RG, Fehlings MG: Pretreatment with calpain inhibitor CEP-4143 inhibits calpain I activation and cytoskeletal degradation, improves neurological function, and enhances axonal survival after traumatic spinal cord injury. J Neurochem 2000 ; 74: 1646-1655.
22. Crocker SJ, Smith PD, Jackson-Lewis V., Lamba WR, Hayley SP, Grimm E.,, et al. Inhibition of calpains prevents neuronal and behavioral deficits in an MPTP mouse model of Parkinson's disease. J Neurosci 2003 ; 23: 4081-4091.
23. Knoblach SM, Alroy DA, Nikolaeva M., Cernak I., Stoica BA, Faden AI: Caspase inhibitor z-DEVD-fmk attenuates calpain and necrotic cell death in vitro and after traumatic brain injury. J Cereb Blood Flow Metab 2004 ; 24: 1119-1132.
24. Shaw E.: Peptidyl diazomethanes as inhibitors of cysteine and serine proteinases. Methods Enzymol 1994 ; 244: 649-656.
25. Zhang JH, Chung TD, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999 ; 4: 67-73.
26. Encinas M., Iglesias M., Liu Y., Wang H., Muhaisen A., Cena V.,, et al. Sequential treatment of SH-SY5Y cells with retinoic acid and brain-derived neurotrophic factor gives rise to fully differentiated, neurotrophic factor-dependent, human neuron-like cells. J Neurochem 2000 ; 75: 991-1003.
27. Simpson PB, Bacha JI, Palfreyman EL, Woollacott AJ, McKernan RM, Kerby J.: Retinoic acid evoked-differentiation of neuroblastoma cells predominates over growth factor stimulation: an automated image capture and quantitation approach to neuritogenesis. Anal Biochem 2001 ; 298: 163-169.