Is It the Twilight of BACEI Inhibitors?

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F21%3A50018771" target="_blank" >RIV/62690094:18470/21:50018771 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/21:00556865 RIV/00179906:_____/21:10426434
Result on the web
<a href="https://www.eurekaselect.net/article/106293" target="_blank" >https://www.eurekaselect.net/article/106293</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.2174/1570159X18666200503023323" target="_blank" >10.2174/1570159X18666200503023323</a>

Result language
angličtina
Original language name
Is It the Twilight of BACEI Inhibitors?
Original language description
beta-secretase (BACE1) has been regarded as a prime target for the development of amyloid beta (A beta) lowering drugs in the therapy of Alzheimer's disease (A beta). Although the enzyme was discovered in 1991 and helped to formulate the AD hypothesis as one of the very important features of A beta etiopathogenesis, progress in A beta treatment utilizing BACE1 inhibitors has remained limited. Moreover, in the last years, major pharmaceutical companies have discontinued clinical trials of five BACE1 inhibitors that had been strongly perceived as prospective. In our review, the A beta hypothesis, the enzyme, its functions, and selected substrates are described. BACE1 inhibitors are classified into four generations. Those that underwent clinical trials displayed adverse effects, including weight loss, skin rashes, worsening of neuropsychiatric symptoms, etc. Some inhibitors could not establish a statistically significant risk-benefit ratio, or even scored worse than placebo. We still believe that drugs targeting BACE1 may still hide some potential, but a different approach to BACE1 inhibition or a shift of focus to modulation of its trafficking and/or post-translational modification should now be followed.
Czech name
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Czech description
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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
30103 - Neurosciences (including psychophysiology)

Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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