Structure-Based Design of Potent and Selective Cell-Permeable Inhibitors of Human β-Secretase (BACE-1)
Shawn J. Stachel(United States Military Academy), Craig A. Coburn(United States Military Academy), Thomas G. Steele(United States Military Academy), Kristen G. Jones(United States Military Academy), Elizabeth F. Loutzenhiser(United States Military Academy), Alison R. Gregro(United States Military Academy), Hemaka A. Rajapakse(United States Military Academy), Ming‐Tain Lai(United States Military Academy), Ming‐Chih Crouthamel(United States Military Academy), Min Xu(United States Military Academy), Katherine Tugusheva(United States Military Academy), Janet Lineberger(United States Military Academy), Beth Pietrak(United States Military Academy), Amy S. Espeseth(United States Military Academy), Xiao‐Ping Shi(United States Military Academy), Elizabeth Chen-Dodson(United States Military Academy), M. Katharine Holloway(United States Military Academy), Sanjeev Munshi(United States Military Academy), Adam J. Simon(United States Military Academy), Lawrence Kuo(United States Military Academy), Joseph P. Vacca(United States Military Academy)
Cited by 276Open Access
Abstract
We describe the development of cell-permeable beta-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.
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