Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2016 Dec 22;22(1):4.
doi: 10.3390/molecules22010004.

Development and Structural Modification of BACE1 Inhibitors

Ting Gu  1 , Wen-Yu Wu  2 , Ze-Xi Dong  3 , Shao-Peng Yu  4 , Ying Sun  5 , Yue Zhong  6 , Yu-Ting Lu  7 , Nian-Guang Li  8
Affiliations
Review

Development and Structural Modification of BACE1 Inhibitors

Ting Gu et al. Molecules. .

Abstract

Alzheimer's disease (AD) is a progressive neurodegenerative disorder which usually occurs in the elderly. The accumulation of β-amyloid and the formation of neurofibrillary tangles are considered as the main pathogenies of AD. Research suggests that β-secretase 1 (BACE1) plays an important role in the formation of β-amyloid. Discovery of new BACE1 inhibitors has become a significant method to slow down the progression of AD or even cure this kind of disease. This review summarizes the different types and the structural modification of these new BACE1 inhibitors.

Keywords: Alzheimer’s disease; BACE1; BACE1 inhibitors; structural modification; β-amyloid.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
BACE1 inhibitors with peptidomimetic structure.
Figure 2
Figure 2
Structures of peptidomimetic BACE1 inhibitors with phenyl groups.
Figure 3
Figure 3
The BACE1 inhibitors with peptidomimetic structures.
Figure 4
Figure 4
BACE1 inhibitors with piperazine rings.
Figure 5
Figure 5
BACE1 inhibitors with amino/imino structures.
Figure 6
Figure 6
Pentatomic ring BACE1 inhibitors with amino structures.
Figure 7
Figure 7
Hexatomic rings BACE1 inhibitors with amino structures.
Figure 8
Figure 8
Structures of curcumin and its derivatives.
Figure 9
Figure 9
Structures of terpenoids.
Figure 10
Figure 10
Structures of alkaloids.
Figure 11
Figure 11
Structures of other natural products.
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. Zhao X.S., Peng J., Wu Q., Ren Z., Pan L.H., Tang Z.H., Jiang Z.S., Wang G.X., Liu L.S. Imbalanced cholesterol metabolism in Alzheimer’s disease. Clin. Chim. Acta. 2016;456:107–114. - PubMed
    1. Oehlrich D., Prokopcova H., Gijsen H.J.M. ChemInform Abstract: The Evolution of Amidine-Based Brain Penetrant BACE1 Inhibitors. Bioorg. Med. Chem. Lett. 2014;45:2033–2045. doi: 10.1016/j.bmcl.2014.03.025. - DOI - PubMed
    1. León R., Garcia A.G., Marco-Contelles J. Recent advances in the multitarget-directed ligands approach for the treatment of Alzheimer’s disease. Med. Chem. Res. 2013;33:139–189. doi: 10.1002/med.20248. - DOI - PubMed
    1. Awasthi M., Singh S., Pandey V.P., Dwivedi U.N. Alzheimer’s disease: An overview of amyloid beta dependent pathogenesis and its therapeutic implications along with in silico approaches emphasizing the role of natural products. J. Neurol. Sci. 2016;361:256–271. doi: 10.1016/j.jns.2016.01.008. - DOI - PubMed
    1. Kaushik A., Jayant R.D., Tiwari S., Vashist A., Nair M. Nano-biosensors to detect beta-amyloid for Alzheimer’s disease management. Biosens. Bioelectron. 2016;80:273–287. doi: 10.1016/j.bios.2016.01.065. - DOI - PMC - PubMed

MeSH terms

LinkOut - more resources