Promising multifunctional anti-Alzheimer's dimer bis(7)-Cognitin acting as an activator of protein kinase C regulates activities of α-secretase and BACE-1 concurrently

European Journal of Pharmacology

Volumn 623, Issue 1-3, 2009, Pages 14-21

  Fu, Hongjun ^a   Dou, Juan ^b   Li, Wenming ^a   Cui, Wei ^a   Mak, Shinghung ^a   Hu, Qiansheng ^b   Luo, Jialie ^a   Lam, Colin S C ^a   Pang, Yuanping ^c   Youdim, Moussa B H ^d   Han, Yifan ^a  

^a HONG KONG POLYTECHNIC UNIVERSITY   (Hong Kong)

^b SUN YAT SEN UNIVERSITY   (China)

^c MAYO CLINIC   (United States)

^d TECHNION ISRAEL INSTITUTE OF TECHNOLOGY   (Israel)

Author keywords

Secretase; Amyloid peptide; BACE 1; Bis(7) Cognitin; Protein kinase C

Indexed keywords

ALPHA SECRETASE; AMYLOID BETA PROTEIN; AMYLOID PRECURSOR PROTEIN; BETA SECRETASE; BIS(7)COGNITIN; CHOLINESTERASE INHIBITOR; PROTEIN KINASE C; UNCLASSIFIED DRUG;

ALZHEIMER DISEASE; ANIMAL CELL; ARTICLE; CHOLINERGIC TRANSMISSION; CONTROLLED STUDY; EMBRYO; ENZYME ACTIVATION; ENZYME ACTIVITY; ENZYME INHIBITION; IN VITRO STUDY; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN PROCESSING; PROTEIN SYNTHESIS INHIBITION; RAT;

ALZHEIMER DISEASE; AMP-ACTIVATED PROTEIN KINASES; AMYLOID BETA-PROTEIN; AMYLOID BETA-PROTEIN PRECURSOR; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; CELL LINE, TUMOR; CELLS, CULTURED; CHOLINESTERASE INHIBITORS; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME ACTIVATORS; HUMANS; MICE; MUSCARINIC ANTAGONISTS; MUTANT PROTEINS; NEURONS; PEPTIDE FRAGMENTS; PHORBOL ESTERS; PROTEIN ISOFORMS; PROTEIN KINASE C; RATS; RECEPTORS, MUSCARINIC; TACRINE;

EID: 70350210477     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2009.09.013     Document Type: Article

References (42)

1. Abbenante G., Kovacs D.M., Leung D.L., Craik D.J., Tanzi R.E., and Fairlie D.P. Inhibitors of beta-amyloid formation based on the beta-secretase cleavage site. Biochem. Biophys. Res. Commun. 268 (2000) 133-135
2. Asai M., Hattori C., Iwata N., Saido T.C., Sasagawa N., Szabó B., Hashimoto Y., Maruyama K., Tanuma S., Kiso Y., and Ishiura S. The novel beta-secretase inhibitor KMI-429 reduces amyloid beta peptide production in amyloid precursor protein transgenic and wild-type mice. J. Neurochem. 96 (2006) 533-540
3. Bolognesi M.L., Rosini M., Andrisano V., Bartolini M., Minarini A., Tumiatti V., and Melchiorre C. MTDL design strategy in the context of Alzheimer's disease: from lipocrine to memoquin and beyond. Curr. Pharm. Des. 15 (2009) 601-613
4. Cai H., Wang Y., McCarthy D., Wen H., Borchelt D.R., Price D.L., and Wong P.C. BACE1 is the major beta-secretase for generation of Abeta peptides by neurons. Nat. Neurosci. 4 (2001) 233-234
5. Citron M. Strategies for disease modification in Alzheimer's disease. Nat. Rev., Neurosci. 5 (2004) 677-685
6. Edwards A., Gillard M., and Merler E. Characterization of muscarinic receptors: type M2 (subtype B) on neuro-2A neuroblastoma cells. J. Recept. Res. 9 (1989) 259-270
7. Fu H., Li W., Lao Y., Luo J., Lee N.T., Kan K.K., Tsang H.W., Tsim K.W., Pang Y., Li Z., Chang D.C., Li M., and Han Y. Bis(7)-tacrine attenuates beta amyloid-induced neuronal apoptosis by regulating L-type calcium channels. J. Neurochem. 98 (2006) 1400-1410
8. Fu H., Li W., Luo J., Lee N.T., Li M., Tsim K.W., Pang Y., Youdim M.B., and Han Y. Promising anti-Alzheimer's dimer bis(7)-tacrine reduces -amyloid generation by directly inhibiting BACE-1 activity. Biochem. Biophys. Res. Commun. 366 (2008) 631-636
9. Hardy J., and Selkoe D.J. The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics. Science 297 (2002) 353-356
10. Hellstrom-Lindahl E. Modulation of beta-amyloid precursor protein processing and tau phosphorylation by acetylcholine receptors. Eur. J. Pharmacol. 393 (2000) 255-263
11. Hooper N.M., and Turner A.J. The search for alpha-secretase and its potential as a therapeutic approach to Alzheimer s disease. Curr. Med. Chem. 9 (2002) 1107-1119
12. Hull M., Berger M., and Heneka M. Disease-modifying therapies in Alzheimer's disease: how far have we come?. Drugs 66 (2006) 2075-2093
13. Kimura T., Shuto D., Hamada Y., Igawa N., Kasai S., Liu P., Hidaka K., Hamada T., Hayashi Y., and Kiso Y. Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability. Bioorg. Med. Chem. Lett. 15 (2005) 211-215
14. Kinouchi T., Sorimachi H., Maruyama K., Mizuno K., Ohno S., Ishiura S., and Suzuki K. Conventional protein kinase C (PKC)-alpha and novel PKC epsilon, but not -delta, increase the secretion of an N-terminal fragment of Alzheimer's disease amyloid precursor protein from PKC cDNA transfected 3Y1 fibroblasts. FEBS Lett. 364 (1995) 203-206
15. Kozikowski A.P., Chen Y., Subhasish T., Lewin N.E., Blumberg P.M., Zhong Z., D'Annibale M.A., Wang W.L., Shen Y., and Langley B. Searching for disease modifiers-PKC activation and HDAC inhibition - a dual drug approach to Alzheimer's disease that decreases Abeta production while blocking oxidative stress. Chem. Med. Chem. 4 (2009) 1095-1105
16. Lee W., Boo J.H., Jung M.W., Park S.D., Kim Y.H., Kim S.U., and Mook-Jung I. Amyloid beta peptide directly inhibits PKC activation. Mol. Cell. Neurosci. 26 (2004) 222-231
17. Li W.M., Pi R., Chan H.H., Fu H., Lee N.T., Tsang H.W., Pu Y., Chang D.C., Li C., Luo J., Xiong K., Li Z., Xue H., Carlier P.R., Pang Y., Tsim K.W., Li M., and Han Y.F. Novel dimeric acetylcholinesterase inhibitor bis7-tacrine, but not donepezil, prevents glutamate-induced neuronal apoptosis by blocking N-methyl-d-aspartate receptors. J. Biol. Chem. 280 (2005) 18179-18188
18. Li W.M., Xue J., Niu C., Fu H., Lam C.S., Luo J., Chan H.H., Xue H., Kan K.K., Lee N.T., Li C., Pang Y., Li M., Tsim K.W., Jiang H., Chen K., Li X., and Han Y.F. Synergistic neuroprotection by bis(7)-tacrine via concurrent blockade of N-methyl-d-aspartate receptors and neuronal nitric-oxide synthase. Mol. Pharmacol. 71 (2007) 1258-1267
19. Li W.M., Mak M., Jiang H., Wang Q., Pang Y., Chen K., and Han Y.F. Novel anti-Alzheimer's dimer bis(7)-Cognitin: cellular and molecular mechanisms of neuroprotection through multiple targets. Neurotherapeutics 6 (2009) 187-201
20. Ma C., Ying C., Yuan Z., Song B., Li D., Liu Y., Lai B., Li W., Chen R., Ching Y.P., and Li M. dp5/HRK is a c-Jun target gene and required for apoptosis induced by potassium deprivation in cerebellar granule neurons. J. Biol. Chem. 282 (2007) 30901-30909
21. Marzolo M.P., and Bu G. Lipoprotein receptors and cholesterol in APP trafficking and proteolytic processing, implications for Alzheimer's disease. Semin. Cell Dev. Biol. 20 (2009) 191-200
22. Nelson T.J., and Alkon D.L. Neuroprotective versus tumorigenic protein kinase C activators. Trends Biochem. Sci. 34 (2009) 136-145
23. Nitsch R.M., Slack B.E., Wurtman R.J., and Growdon J.H. Release of Alzheimer amyloid precursor derivatives stimulated by activation of muscarinic acetylcholine receptors. Science 258 (1992) 304-307
24. Pang Y.P., Quiram P., Jelacic T., Hong F., and Brimijoin S. Highly potent, selective, and low cost bis-tetrahydroaminacrine inhibitors of acetylcholinesterase. Steps toward novel drugs for treating Alzheimer's disease. J. Biol. Chem. 271 (1996) 23646-23649
25. Peng Y., Lee D.Y., Jiang L., Ma Z., Schachter S.C., and Lemere C.A. Huperzine A regulates amyloid precursor protein processing via protein kinase C and mitogen-activated protein kinase pathways in neuroblastoma SK-N-SH cells over-expressing wild type human amyloid precursor protein 695. Neuroscience 150 (2007) 386-395
26. Pereira C., Agostinho P., Moreira P.I., Cardoso S.M., and Oliveira C.R. Alzheimer's disease-associated neurotoxic mechanisms and neuroprotective strategies. Curr. Drug Targets CNS Neurol. Disord. 4 (2005) 383-403
27. Racchi M., Mazzucchelli M., Lenzken S.C., Porrello E., Lanni C., and Govoni S. Role of acetylcholinesterase inhibitors in the regulation of amyloid beta precursor protein (AbetaPP) metabolism. Chem. Biol. Interact. 157-158 (2005) 335-338
28. Roberson E.D., and Mucke L. 100 years and counting: prospects for defeating Alzheimer's disease. Science 314 (2006) 781-784
29. Savage M.J., Trusko S.P., Howland D.S., Pinsker L.R., Mistretta S., Reaume A.G., Greenberg B.D., Siman R., and Scott R.W. Turnover of amyloid beta-protein in mouse brain and acute reduction of its level by phorbol ester. J. Neurosci. 18 (1998) 1743-1752
30. Sun M.K., and Alkon D.L. Protein kinase C isozymes: memory therapeutic potential. Curr. Drug Targets CNS Neurol. Disord. 4 (2005) 541-552
31. Teo J.L., Ma H., Nguyen C., Lam C., and Kahn M. Specific inhibition of CBP/beta-catenin interaction rescues defects in neuronal differentiation caused by a presenilin-1 mutation. Proc. Natl. Acad. Sci. U. S. A. 102 (2005) 12171-12176
32. Thinakaran G., Teplow D.B., Siman R., Greenberg B., and Sisodia S.S. Metabolism of the "Swedish" amyloid precursor protein variant in neuro2a (N2a) cells. Evidence that cleavage at the "beta-secretase" site occurs in the golgi apparatus. J. Biol. Chem. 271 (1996) 9390-9397
33. Van der Schyf C.J., Mandel S., Geldenhuys W.J., Amit T., Avramovich Y., Zheng H., Fridkin M., Gal S., Weinreb O., Bar Am O., Sagi Y., and Youdim M.B. Novel multifunctional anti-Alzheimer drugs with various CNS neurotransmitter targets and neuroprotective moieties. Curr. Alzheimer Res. 4 (2007) 522-536
34. Wang L., Shim H., Xie C., and Cai H. Activation of protein kinase C modulates BACE-1 mediated beta-secretase activity. Neurobiol. Aging 29 (2008) 357-367
35. Weinreb O., Bar-Am O., Amit T., Chillag-Talmor O., and Youdim M.B. Neuroprotection via pro-survival protein kinase C isoforms associated with Bcl-2 family members. FASEB J. 18 (2004) 1471-1473
36. Yang H.Q., Pan J., Ba M.W., Sun Z.K., Ma G.Z., Lu G.Q., Xiao Q., and Chen S.D. New protein kinase C activator regulates amyloid precursor protein processing in vitro by increasing alpha-secretase activity. Eur. J. Neurosci. 26 (2007) 381-391
37. Yogev-Falach M., Amit T., Bar-Am O., Weinstock M., and Youdim M.B. Involvement of MAP kinase in the regulation of amyloid precursor protein processing by novel cholinesterase inhibitors derived from rasagiline. FASEB J. 16 (2002) 1674-1676
38. Yogev-Falach M., Amit T., Bar-Am O., and Youdim M.B. The importance of propargylamine moiety in the anti-Parkinson drug rasagiline and its derivatives in MAPK-dependent amyloid precursor protein processing. FASEB J. 17 (2003) 2325-2327
39. Youdim M.B., and Buccafusco J.J. CNS Targets for multi-functional drugs in the treatment of Alzheimer's and Parkinson's diseases. J. Neural Transm. 112 (2005) 519-537
40. Zhang H.Y. One-compound-multiple-targets strategy to combat Alzheimer's disease. FEBS Lett. 579 (2005) 5260-5264
41. Zhang H.Y., and Tang X.C. Neuroprotective effects of huperzine A: new therapeutic targets for neurodegenerative disease. Trends Pharmacol. Sci. 27 (2006) 619-625
42. Zimmermann M., Gardoni F., Marcello E., Colciaghi F., Borroni B., Padovani A., Cattabeni F., and Di Luca M. Acetylcholinesterase inhibitors increase ADAM10 activity by promoting its trafficking in neuroblastoma cell lines. J. Neurochem. 90 (2004) 1489-1499