The DOI matches its Crossref record; 8 of the 8 references it cites were found in a registry or an index.
Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment
Open accessAbstract
Alzheimer's disease (AD) is a severe neurodegenerative disorder and the most common type of dementia in the elderly. The clinical symptoms of AD include a progressive loss of memory and impairment of cognitive functions interfering with daily life activities. The main neuropathological features consist in extracellular amyloid-β (Aβ) plaque deposition and intracellular Neurofibrillary tangles (NFTs) of hyperphosphorylated Tau. Understanding the pathophysiological mechanisms that underlie neurodegeneration in AD is essential for rational design of neuroprotective agents able to prevent disease progression. According to the "Amyloid Cascade Hypothesis" the critical molecular event in the pathogenesis of AD is the accumulation of Aβ neurotoxic oligomers. Since the proteolytic processing of Amyloid Precursor Protein (APP) by β-secretase (beta-site APP cleaving enzyme 1, BACE1) is the rate-limiting step in the production of Aβ, this enzyme is considered a major therapeutic target and BACE1 inhibitors have the potential to be disease-modifying drugs for AD treatment. Therefore, intensive efforts to discover and develop inhibitors that can reach the brain and effectively inhibit BACE1 have been pursued by several groups worldwide. The aim of this review is to highlight the progress in the discovery of potent and selective small molecule BACE1 inhibitors over the past decade.
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Cites
The amyloid hypothesis of Alzheimer's disease at 25 years
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“Since BACE1 identification in 1999 (Vassar, 1999), inhibitors covering many different structural classes have been extensively reported in the literature (Ghosh et al., 2012; Ghosh and Osswald, 2014; Menting and Claassen, 2014; Yan and Vassar, 2014).”
BackgroundKarran, E., Mercken, M., & Strooper, B. D. (2011) · Nature Reviews Drug Discovery · doi:10.1038/nrd3505 · Cited by 2,188 · cited 1×
“The “Amyloid Cascade Hypothesis” proposes that the cerebral appearance of aggregates of oligomeric Aβ plays a central role for AD neuropathogenicity (Karran et al., 2011; Selkoe and Hardy, 2016).”
BackgroundAlzheimer's disease drug development pipeline: 2017
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Modulation of γ- and β-secretases as early prevention against Alzheimer's disease
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Exosomes — beyond stem cells for restorative therapy in stroke and neurological injury
Zhang, Z. G., Buller, B., & Chopp, M. (2019) · Nature Reviews Neurology · doi:10.1038/s41582-018-0126-4 · Cited by 503
Webers, A., Heneka, M. T., & Gleeson, P. A. (2020) · Immunology & Cell Biology · doi:10.1111/imcb.12301 · Cited by 367
Sharma, P., Srivastava, P., Seth, A., Tripathi, P. N., Banerjee, A. G., & Shrivastava, S. K. (2019) · Progress in Neurobiology · doi:10.1016/j.pneurobio.2018.12.006 · Cited by 331
BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease
Moussa‐Pacha, N. M., Abdin, S. M., Omar, H. A., Alniss, H., & Al‐Tel, T. H. (2020) · Medicinal Research Reviews · doi:10.1002/med.21622 · Cited by 274
Investigational BACE inhibitors for the treatment of Alzheimer’s disease
Imbimbo, B. P., & Watling, M. (2019) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2019.1683160 · Cited by 132
Metadata
- Authors
- Coimbra, J. R. M., Marques, D. F. F., Baptista, S. J., Pereira, C. M. F., Moreira, P. I., Dinis, T. C. P., Santos, A. E., & Salvador, J. A. R.
- Venue
- Frontiers in Chemistry
- Publisher
- Frontiers Media SA
- Published
- 2018-05-24
- Volume
- 6
- Pages
- 178-178
- ISSN
- 2296-2646 (ISSN-L)
- OpenAlex
- W2800986210
- Cited by
- 171
- References
- 8
- FWCI
- 14.10
- Type
- journal article
- Language
- en
- Open access
- gold
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- Coimbra, J. R. M., Marques, D. F. F., Baptista, S. J., Pereira, C. M. F., Moreira, P. I., Dinis, T. C. P., Santos, A. E., & Salvador, J. A. R. (2018). Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment. Frontiers in Chemistry. https://doi.org/10.3389/fchem.2018.00178
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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