Chemistry Reference
In-Depth Information
[4] Roberds, S. L., Anderson, J., Basi, G., Bienkowski, M. J., Branstetter, D. G., Chen, K. S.,
Freedman, S. B., Frigon, N. L., Games, D., Hu, K., Johnson-Wood, K., Kappenman, K. E.,
Kawabe, T. T., Kola, I., Kuehn, R., Lee, M., Liu, W., Motter, R., Nichols, N. F., Power, M.,
Robertson, D.W., Schenk, D., Schoor,M., Shopp, G.M., Shuck,M. E., Sinha, S., Svensson, K.A.,
Tatsuno, G., Tintrup, H., Wijsman, J., Wright, S., McConlogue, L. BACE knockout mice are
healthy despite lacking the primary -secretase activity in brain: implications for Alzheimer's
disease therapeutics. Hum. Mol. Genet. 2001, 10 , 1317-1324.
[5] Luo, Y., Bolon, B., Kahn, S., Bennett, B. D., Babu-Khan, S., Denis, P., Fan, W., Kha, H.,
Zhang, J., Gong, Y., Martin, L., Louis, J.-C., Yan, Q., Richards, W. G., Citron, M., Vassar, R.
Mice deficient in BACE1, the Alzheimer's -secretase, have normal phenotype and abolished
-amyloid generation. Nat. Neurosci. 2001, 4 , 231-232.
[6] Harrison, S. M., Harper, A. J., Hawkins, J., Duddy, G., Grau, E., Pugh, P. L., Winter, P. H., Shil-
liam, C. S., Hughes, Z.A., Dawson, L.A., Gonzalez, M. I., Upton, N., Pangalos, M. N., Dingwall,
C. BACE1 (-secretase) transgenic and knockout mice: identification of neurochemical deficits
and behavioral changes. Mol. Cell. Neurosci. 2003, 24 , 646-655.
[7] Vassar, R., Bennett, B. D., Babu-Khan, S., Kahn, S., Mendiaz, E. A., Denis, P., Teplow, D. B.,
Ross, S., Amarante, P., Loeloff, R., Luo, Y., Fisher, S., Fuller, J., Edenson, S., Lile, J., Jarosinski,
M. A., Biere, A. L., Curran, E., Burgess, T., Louis, J.-C., Collins, F., Treanor, J., Rogers, G.,
Citron,M. -Secretase cleavage ofAlzheimer's amyloid precursor protein by the transmembrane
aspartic protease BACE. Science 1999, 286 , 735-741.
[8] Sinha, S., Anderson, J. P., Barbour, R., Basi, G. S., Caccavello, R., Davis, D., Doan, M., Dovey,
H. F., Frigon, N., Hong, J., Jacobson-Croak, K., Jewett, N., Keim, P., Knops, J., Lieberburg, I.,
Power, M., Tan, H., Tatsuno, G., Tung, J., Schenk, D., Seubert, P., Suomensaari, S. M., Wang, S.,
Walker, D., Zhao, J., McConlogue, L., John, V. Purification and cloning of amyloid precursor
protein -secretase from human brain. Nature 1999, 402 , 537-540.
[9] Yan, R., Bienkowski, M. J., Shuck, M. E., Miao, H., Tory, M. C., Pauley, A. M., Brashler, J. R.,
Stratman, N. C., Mathews,W. R., Buhl,A. E., Carter, D. B., Tomasselli,A. G., Parodi, L.A., Hein-
rikson, R. L., Gurney, M. E. Membrane-anchored aspartyl protease with Alzheimer's disease
-secretase activity. Nature 1999, 402 , 533-537.
[10] Hussain, I., Powell, D., Howlett, D. R., Tew, D. G., Meek, T. D., Chapman, C., Gloger, I. S.,
Murphy, K. E., Southan, C. D., Ryan, D. M., Smith, T. S., Simmons, D. L., Walsh, F. S.,
Dingwall, C., Christie, G. Identification of a novel aspartic protease (Asp 2) as -secretase. Mol.
Cell. Neurosci. 1999, 14 , 419-427.
[11] Lin, X., Koelsch, G., Wu, S., Downs, D., Dashti, A., Tang, J. Human aspartic protease memapsin
2 cleaves the -secretase site of -amyloid precursor protein. Proc. Natl. Acad. Sci. USA 2000,
97 , 1456-1460.
[12] Durham, T. B., Shepherd, T. A. Progress toward the discovery and development of efficacious
BACE inhibitors. Curr. Opin. Drug Discov. Dev. 2006, 9 , 776-791.
[13] Baxter, E. W., Reitz, A. B. BACE inhibitors for the treatment of Alzheimer's disease. Annu.
Rep. Med. Chem. 2005, 40 , 35-48.
[14] Schmidt, B., Baumann, S., Braun, H. A., Larbig, G. Inhibitors and modulators of - and
-secretase. Curr. Top. Med. Chem. 2006, 6 , 377-392.
[15] Guo, T., Hobbs, D. W. Development of BACE1 inhibitors for Alzheimer's disease. Curr. Med.
Chem. 2006, 13 , 1811-1829.
[16] Ghosh, A. K., Kumaragurubaran, N., Tang, J. Recent developments of structure-based
-secretase inhibitors for Alzheimer's disease. Curr. Top. Med. Chem. 2005, 5 , 1609-1622.
[17] Hong, L., Koelsch, G., Lin, X.,Wu, S., Terzyan, S., Ghosh,A. K., Zhang, X. C., Tang, J. Structure
of the protease domain of memapsin 2 (-secretase) complexed with inhibitor. Science 2000,
290 , 150-153.
Search WWH ::




Custom Search