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 |
|---|
| 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 |
|---|
| Vrsta gradiva: | Članek v reviji |
|---|
| Tipologija: | 1.01 - Izvirni znanstveni članek |
|---|
| Organizacija: | FFA - Fakulteta za farmacijo
|
|---|
| Status publikacije: | Objavljeno |
|---|
| Različica publikacije: | Objavljena publikacija |
|---|
| Leto izida: | 2016 |
|---|
| Št. strani: | 11 str. |
|---|
| Številčenje: | Vol. 9, iss. 1, art. 2 |
|---|
| PID: | 20.500.12556/RUL-130387  |
|---|
| UDK: | 543:615.2 |
|---|
| ISSN pri članku: | 1424-8247 |
|---|
| DOI: | 10.3390/ph9010002 |
|---|
| COBISS.SI-ID: | 4018289 |
|---|
| Datum objave v RUL: | 14.09.2021 |
|---|
| Število ogledov: | 1172 |
|---|
| Število prenosov: | 159 |
|---|
| Metapodatki: |    |
|---|
|
:
|
Kopiraj citat |
|---|
| Objavi na: |  |
|---|
