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Development of potent reversible selective inhibitors of butyrylcholinesterase as fluorescent probesPajk, Stane, 1983- ...Brain butyrylcholinesterase (BChE) is an attractive target for drugs designed for the treatment of Alzheimer's disease (AD) in its advanced stages. It also potentially represents a biomarker for ... progression of this disease. Based on the crystal structure of previously described highly potent, reversible, and selective BChE inhibitors, we have developed the fluorescent probes that are selective towards human BChE. The most promising probes also maintain their inhibition of BChE in the low nanomolar range with high selectivity over acetylcholinesterase. Kinetic studies of probes reveal a reversible mixed inhibition mechanism, with binding of these fluorescent probes to both the free and acylated enzyme. Probes show environment-sensitive emission, and additionally, one of them also shows significant enhancement of fluorescence intensity upon binding to the active site of BChE. Finally, the crystal structures of probes in complex with human BChE are reported, which offer an excellent base for further development of this library of compounds.Source: Journal of enzyme inhibition and medicinal chemistry. - ISSN 1475-6366 (Vol. 35, iss. 1, 2020, str. 498-505)Type of material - article, component partPublish date - 2020Language - englishCOBISS.SI-ID - 4869233
Author
Pajk, Stane, 1983- |
Knez, Damijan, farmacevt |
Košak, Urban |
Zorović, Maja |
Brazzolotto, Xavier |
Coquelle, Nicolas |
Nachon, Florian |
Colletier, Jacques-Philippe |
Živin, Marko, 1958- |
Stojan, Jure, 1956- |
Gobec, Stanislav, 1970-
Topics
Alzheimerjeva bolezen |
Demenca |
butyrylcholinesterase |
inhibitor |
probe |
fluorescence |
patogeneza Alzheimerjeve bolezni |
butiriliholinesteraza |
zaviralci
source: Journal of enzyme inhibition and medicinal chemistry. - ISSN 1475-6366 (Vol. 35, iss. 1, 2020, str. 498-505)
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Pajk, Stane, 1983- | 28861 |
Knez, Damijan, farmacevt | 36438 |
Košak, Urban | 33908 |
Zorović, Maja | 21503 |
Brazzolotto, Xavier | |
Coquelle, Nicolas | |
Nachon, Florian | |
Colletier, Jacques-Philippe | |
Živin, Marko, 1958- | 08289 |
Stojan, Jure, 1956- | 03723 |
Gobec, Stanislav, 1970- | 15284 |
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