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3,1-benzothiazines, 1,4-benzodioxines, 1,4-benzoxazines as inhibitors of matriptase-2 [Elektronski vir] : outcome of a focused screening approachRoydeva, Polya G. ...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 %-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 IC50 value of less than 10 %M. Structure-activity relationships were discussed and proposals to design new matriptase-2 inhibitors were made.Vir: Pharmaceuticals [Elektronski vir]. - ISSN 1424-8247 (Vol. 9, issue. 1, 2016, 11 str.)Vrsta gradiva - e-članek ; neleposlovje za odrasleLeto - 2016Jezik - angleškiCOBISS.SI-ID - 4018289
Povezava(-e):
http://www.mdpi.com/1424-8247/9/1/2Prosti dostop
Repozitorij Univerze v Ljubljani – RUL
DOI
Avtor
Roydeva, Polya G. |
Beckmann, Anna-Madeleine |
Stirnberg, Marit |
Cesar, Jožko |
Kikelj, Danijel |
Ilaš, Janez |
Gütschow, Michael
Teme
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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Baze podatkov, v katerih je revija indeksirana
Ime baze podatkov | Področje | Leto |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Roydeva, Polya G. | |
Beckmann, Anna-Madeleine | |
Stirnberg, Marit | |
Cesar, Jožko | 19062 |
Kikelj, Danijel | 01463 |
Ilaš, Janez | 24400 |
Gütschow, Michael |
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