Autor: |
Stachel, S. J., Coburn, C. A., Steele, T. G., Jones, K. G., Loutzenhiser, E. F., Gregro, A. R., Rajapakse, H. A., Lai, M.-T., Crouthamel, M.-C., Xu, M., Tugusheva, K., Lineberger, J. E., Pietrak, B. L., Espeseth, A. S., Shi, X.-P., Chen-Dodson, E., Holloway, M. K., Munshi, S., Simon, A. J., Kuo, L., Vacca, J. P. |
Zdroj: |
Journal of Medicinal Chemistry; December 2004, Vol. 47 Issue: 26 p6447-6450, 4p |
Abstrakt: |
We describe the development of cell-permeable β-secretase inhibitors that demonstratively inhibit the production of the secreted amino terminal fragment of an artificial amyloid precursor protein in cell culture. In addition to potent inhibition in a cell-based assay (IC50 < 100 nM), these inhibitors display impressive selectivity against other biologically relevant aspartyl proteases. |
Databáze: |
Supplemental Index |
Externí odkaz: |
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