Multitarget tacrine hybrids with neuroprotective properties to confront Alzheimer's disease
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00023752%3A_____%2F17%3A43919250" target="_blank" >RIV/00023752:_____/17:43919250 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/17:43889387 RIV/00179906:_____/17:10338063
Result on the web
<a href="http://www.eurekaselect.com/145857/article" target="_blank" >http://www.eurekaselect.com/145857/article</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.2174/1568026605666160927152728" target="_blank" >10.2174/1568026605666160927152728</a>
Alternative languages
Result language
angličtina
Original language name
Multitarget tacrine hybrids with neuroprotective properties to confront Alzheimer's disease
Original language description
Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder. Several hallmarks such as β-amyloid (Aβ) aggregation underlying amyloid plaque formation, τ-hyperphosphorylation leading to production of neurofibrillary tangles, and decline in the number of cholinergic neurons appear to be fundamental in the pathophysiology of the disease. Other evidence points also to the involvement of oxidative stress, biometal dyshomeostasis, inflammation, and cell cycle regulatory failure. Taking into account such premises, many attractive targets for the development of anti-AD drugs have emerged. Specifically, the multifactorial nature of AD calls for multi-target-directed ligands (MTDLs) which can be beneficial by providing interactions with multiple targets. Tacrine (THA), the first clinically effective acetylcholinesterase inhibitor, was approved for the treatment of mild to moderate AD. Unfortunately, frequent adverse effects including peripheral cholinergic effects and hepatotoxicity limited its therapeutic potential. Based on the numerous biological systems involved in AD progression, this review covers THA-incorporated hybrids possessing a neuroprotective profile. In particular, it focuses on THA hybrids capable of scavenging reactive oxygen species (ROS), and derivatives which reduce the formation of Aβ-plaques either directly by confronting the Aβ1-42 selfaggregation process or indirectly by inhibiting the BACE-1 enzyme or AChE-induced Aβ1-40 aggregation. Particular interest is also addressed to THA hybrids with suppressed hepatotoxicity.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10608 - Biochemistry and molecular biology
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Current Topics in Medicinal Chemistry
ISSN
1568-0266
e-ISSN
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Volume of the periodical
17
Issue of the periodical within the volume
9
Country of publishing house
NL - THE KINGDOM OF THE NETHERLANDS
Number of pages
21
Pages from-to
1006-1026
UT code for WoS article
000394571200004
EID of the result in the Scopus database
2-s2.0-85013797993