BACE inhibitors as potential therapeutics for Alzheimer's disease.
Author
Evin, G; Kenche, VBDate
2007-11Source Title
Recent Pat CNS Drug DiscovPublisher
Bentham Science Publishers Ltd.Affiliation
PathologyMetadata
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Journal ArticleCitations
Evin, G. & Kenche, V. B. (2007). BACE inhibitors as potential therapeutics for Alzheimer's disease.. Recent Pat CNS Drug Discov, 2 (3), pp.188-199. https://doi.org/10.2174/157488907782411783.Access Status
This item is currently not available from this repositoryDescription
C1 - Journal Articles Refereed
Abstract
Accumulation of Abeta peptide in the brain results in the formation of amyloid plaques characteristic of Alzheimer's disease (AD) pathology. Abeta soluble oligomers and protofibrils are neurotoxic and these are believed to be a major cause of neurodegeneration in AD. Abeta is derived from a precursor protein by two sequential cleavage steps involving beta- and gamma-secretases, two proteolytic enzymes that represent rational drug targets. beta-secretase was identified as the membrane-anchored aspartyl protease BACE (or BACE1) and found to be elevated in brain cortex of patients with sporadic Alzheimer's disease. In this review, we summarize current approaches towards the development of BACE inhibitors with focus on bioactive compounds and related patents. Recent reports have described drugs that are effective at inhibiting Abeta production in the brain of transgenic mouse models. The beginning of Phase I clinical trials has been approved for one of them and we can expect that in the near future BACE inhibitors will provide novel effective therapeutics to treat AD.
Keywords
Neurology and Neuromuscular Diseases; Neurodegenerative Disorders Related to AgeingExport Reference in RIS Format
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