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Cited by 358

The DOI matches its Crossref record; 191 of the 191 references it cites were found in a registry or an index.

BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's disease

Open access
Ghosh, Arun K., Osswald, Heather L.·2014·Chem. Soc. Rev.

Abstract

BACE1 (β-secretase, memapsin 2, Asp2) has emerged as a promising target for the treatment of Alzheimer's disease. BACE1 is an aspartic protease which functions in the first step of the pathway leading to the production and deposition of amyloid-β peptide (Aβ). Its gene deletion showed only mild phenotypes. BACE1 inhibition has direct implications in the Alzheimer's disease pathology without largely affecting viability. However, inhibiting BACE1 selectively in vivo has presented many challenges to medicinal chemists. Since its identification in 2000, inhibitors covering many different structural classes have been designed and developed. These inhibitors can be largely classified as either peptidomimetic or non-peptidic inhibitors. Progress in these fields resulted in inhibitors that contain many targeted drug-like characteristics. In this review, we describe structure-based design strategies and evolution of a wide range of BACE1 inhibitors including compounds that have been shown to reduce brain Aβ, rescue the cognitive decline in transgenic AD mice and inhibitor drug candidates that are currently in clinical trials.

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Metadata

Authors
Ghosh, A. K., & Osswald, H. L.
Venue
Chem. Soc. Rev.
Published
2014-04-02
Volume
43
Issue
19
Pages
6765-6813
ISSN
  • 0306-0012 (ISSN-L)
  • 1460-4744
OpenAlex
W2076658253
Cited by
358
References
191
FWCI
4.97
Type
journal article
Language
en
Open access
green

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CoChat. (2026). Citation check: BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's disease. https://app.cochat.ai/papers/10.1039/c3cs60460h
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Ghosh, A. K., & Osswald, H. L. (2014). BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's disease. Chem. Soc. Rev. https://doi.org/10.1039/c3cs60460h

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.