The liver enzyme matriptase-2 is a multi-domain, transmembrane serine protease with an extracellular, C-terminal catalytic domain. Synthetic low-molecular weight inhibitors of matriptase-2 have potential as therapeutics to treat iron overload syndromes, in particular in patients with β-thalassemia. A sub-library of 64 compounds was screened for matriptase-2 inhibition and several active compounds were identified. (S)-Ethyl 2-(benzyl(3-((4-carbamidoylphenoxy)methyl)-2,3-dihydrobenzo[b][1,4]dioxin-6-yl)amino)-2-oxoacetate ((S)-12) showed an IC$_{50}$ value of less than 10 µM. Structure-activity relationships were discussed and proposals to design new matriptase-2 inhibitors were made.
| Jezik: | Angleški jezik |
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| Ključne besede: | marine alkaloid, Agelas, clathrodin, oroidin, pyrrole-2-aminoimidazole, antibacterial, benzamidines, 4H-3, 1-benzothiazin-4-ones, 2, 3-dihydro-1, 4-benzodioxines, 3, 4-dihydro-2H-1, 4-benzoxazines, matriptase-2, protease inhibition |
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| Vrsta gradiva: | Članek v reviji |
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| Tipologija: | 1.01 - Izvirni znanstveni članek |
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| Organizacija: | FFA - Fakulteta za farmacijo
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| Status publikacije: | Objavljeno |
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| Različica publikacije: | Objavljena publikacija |
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| Leto izida: | 2016 |
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| Št. strani: | 11 str. |
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| Številčenje: | Vol. 9, iss. 1, art. 2 |
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| PID: | 20.500.12556/RUL-130387  |
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| UDK: | 543:615.2 |
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| ISSN pri članku: | 1424-8247 |
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| DOI: | 10.3390/ph9010002 |
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| COBISS.SI-ID: | 4018289 |
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| Datum objave v RUL: | 14.09.2021 |
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| Število ogledov: | 819 |
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| Število prenosov: | 132 |
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| Metapodatki: |     |
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