Article ; Online: A method for the efficient evaluation of substrate-based cholinesterase imaging probes for Alzheimer's disease.
Journal of enzyme inhibition and medicinal chemistry
2023 Volume 38, Issue 1, Page(s) 2225797
Abstract: Cholinesterase (ChE) enzymes have been identified as diagnostic markers for Alzheimer disease (AD). Substrate-based probes have been synthesised to detect ChEs but they have not detected changes in ChE distribution associated with AD pathology. Probes ... ...
| Abstract | Cholinesterase (ChE) enzymes have been identified as diagnostic markers for Alzheimer disease (AD). Substrate-based probes have been synthesised to detect ChEs but they have not detected changes in ChE distribution associated with AD pathology. Probes are typically screened using spectrophotometric methods with pure enzyme for specificity and kinetics. However, the biochemical properties of ChEs associated with AD pathology are altered. The present work was undertaken to determine whether the Karnovsky-Roots (KR) histochemical method could be used to evaluate probes at the site of pathology. Thirty thioesters and esters were synthesised and evaluated using enzyme kinetic and KR methods. Spectrophotometric methods demonstrated all thioesters were ChE substrates, yet only a few provided staining in the brain with the KR method. Esters were ChE substrates with interactions with brain ChEs. These results suggest that the KR method may provide an efficient means to screen compounds as probes for imaging AD-associated ChEs. |
|---|---|
| MeSH term(s) | Humans ; Cholinesterases/metabolism ; Alzheimer Disease/diagnostic imaging ; Cholinesterase Inhibitors/chemistry ; Brain ; Acetylcholinesterase/metabolism |
| Chemical Substances | Cholinesterases (EC 3.1.1.8) ; Cholinesterase Inhibitors ; 2-(N-cyclohexylamino)ethanesulfonic acid (103-47-9) ; Acetylcholinesterase (EC 3.1.1.7) |
| Language | English |
| Publishing date | 2023-06-26 |
| Publishing country | England |
| Document type | Journal Article |
| ZDB-ID | 2082578-X |
| ISSN | 1475-6374 ; 1475-6366 |
| ISSN (online) | 1475-6374 |
| ISSN | 1475-6366 |
| DOI | 10.1080/14756366.2023.2225797 |
| Database | MEDical Literature Analysis and Retrieval System OnLINE |
More links
Kategorien
In stock of ZB MED Cologne/Königswinter
| Zs.A 3004: Show issues | Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular Jg. 1995 - 2021: Lesesall (2.OG) ab Jg. 2022: Lesesaal (EG) |
Order via subito
This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.