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Stereoselective activity of 1-propargyl-4-styrylpiperidine-like analogues that can discriminate between monoamine oxidase isoforms A and BKnez, Damijan, farmacevt ...The resurgence of interest in monoamine oxidases (MAOs) has been fueled by recent correlations of this enzymatic activity with cardiovascular, neurological, and oncological disorders. This has ... promoted increased research into selective MAO-A and MAO-B inhibitors. Here, we shed light on how selective inhibition of MAO-A and MAO-B can be achieved by geometric isomers of cis- and trans-1-propargyl-4-styrylpiperidines. While the cis isomers are potent human MAO-A inhibitors, the trans analogues selectively target only the MAO-B isoform. The inhibition was studied by kinetic analysis, UV-vis spectrum measurements, and X-ray crystallography. The selective inhibition of the MAO-A and MAO-B isoforms was confirmed ex vivo in mouse brain homogenates, and additional in vivo studies in mice show the therapeutic potential of 1-propargyl-4-styrylpiperidines for central nervous system disorders. This study represents a unique case of stereoselective activity of cis/trans isomers that can discriminate between structurally related enzyme isoforms.Source: Journal of medicinal chemistry. - ISSN 0022-2623 (Vol. 63, iss. 3, 2020, str. 1361-1387)Type of material - article, component partPublish date - 2020Language - englishCOBISS.SI-ID - 4872561
Author
Knez, Damijan, farmacevt |
Colettis, Natalia |
Iacovino, Luca G. |
Sova, Matej, 1979- |
Pišlar, Anja |
Konc, Janez |
Lešnik, Samo |
Higgs, Josefina |
Kamecki, Fabiola |
Mangialavori, Irene |
Dolšak, Ana, farmacevtka, 1993- |
Žakelj, Simon |
Trontelj, Jurij |
Kos, Janko, 1959- |
Binda, Claudia |
Marder Mariel, Nora |
Gobec, Stanislav, 1970-
Topics
Encimska aktivnost |
razvoj zdravil |
toksikologija zdravil |
monoamin oksidaze
Author | Knez, Damijan, farmacevt ... |
Title | Stereoselective activity of 1-propargyl-4-styrylpiperidine-like analogues that can discriminate between monoamine oxidase isoforms A and B |
Publication date | 2020-01-28 |
COBISS.SI-ID | 4872561 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
---|---|---|---|
Razvoj multifunkcionalnih učinkovin za zdravljenje Alzheimerjeve bolezni | L1-8157-2017 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Novi pristopi za boljša biološka zdravila | L7-8269-2017 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Farmacevtska biotehnologija: znanost za zdravje | P4-0127-2019 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b01886 |
https://repozitorij.uni-lj.si/IzpisGradiva.php?id=141341 |
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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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Knez, Damijan, farmacevt | 36438 |
Colettis, Natalia | |
Iacovino, Luca G. | |
Sova, Matej, 1979- | 25490 |
Pišlar, Anja | 32035 |
Konc, Janez | 25435 |
Lešnik, Samo | 37452 |
Higgs, Josefina | |
Kamecki, Fabiola | |
Mangialavori, Irene | |
Dolšak, Ana, farmacevtka, 1993- | 50400 |
Žakelj, Simon | 22659 |
Trontelj, Jurij | 23420 |
Kos, Janko, 1959- | 04648 |
Binda, Claudia | |
Marder Mariel, Nora | |
Gobec, Stanislav, 1970- | 15284 |
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