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Cited by 262

The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.

Structure-Based Design of Potent and Selective Cell-Permeable Inhibitors of Human β-Secretase (BACE-1)

Stachel, Shawn J., Coburn, Craig A., Steele, Thomas G., Jones, Kristen G., Loutzenhiser, Elizabeth F., Gregro, Alison R., Rajapakse, Hemaka A., Lai, Ming-Tain, Crouthamel, Ming-Chih, Xu, Min, Tugusheva, Katherine, Lineberger, Janet E., Pietrak, Beth L., Espeseth, Amy S., Shi, Xiao-Ping, Chen-Dodson, Elizabeth, Holloway, M. Katharine, Munshi, Sanjeev, Simon, Adam J., Kuo, Lawrence, Vacca, Joseph P.·2004·Journal of Medicinal Chemistry
DOI 10.1021/jm049379g
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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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Crossref · 10.1021/jm049379g

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1 of 1 references verified0 citation errors · 0 not checkable

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  • Treatment of primary neurons with BACE1 inhibitor C3 strongly reduced sSEZ6L levels compared to control, with a concomitant moderate increase of full-length SEZ6L levels in the cell lysate.

    “In fact, treatment of primary neurons with the established BACE1 inhibitor C3 (also known as BACE1 inhibitor IV) [35] strongly reduced sSEZ6L levels compared to the control treatment with a concomitant moderate increase of full-length SEZ6L levels in the cell lysate (Fig. 2b).”

    From Seizure protein 6 and its homolog seizure 6-like protein are physiological substrates of BACE1 in neurons (2016) · cites this paper as [35]

Citations

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Research works printed but not linked: 26

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Metadata

Authors
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.
Venue
Journal of Medicinal Chemistry
Publisher
American Chemical Society (ACS)
Published
2004-11-11
Volume
47
Issue
26
Pages
6447-6450
ISSN
  • 0022-2623
  • 1520-4804
DOI
10.1021/jm049379g
Cited by
262
References
1
Language
en

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