Academic Journal
Design and chemical syntheses of potent matriptase‐2 inhibitors based on trypsin inhibitor SFTI‐1 isolated from sunflower seeds
| العنوان: | Design and chemical syntheses of potent matriptase‐2 inhibitors based on trypsin inhibitor SFTI‐1 isolated from sunflower seeds |
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| المؤلفون: | Gitlin‐Domagalska, Agata, Dębowski, Dawid, Łęgowska, Anna, Stirnberg, Marit, Okońska, Joanna, Gütschow, Michael, Rolka, Krzysztof |
| المساهمون: | National Science Centre, German Research Foundation |
| المصدر: | Peptide Science ; volume 108, issue 6 ; ISSN 0006-3525 |
| بيانات النشر: | Wiley |
| سنة النشر: | 2017 |
| المجموعة: | Wiley Online Library (Open Access Articles via Crossref) |
| الوصف: | Matriptase‐2 plays a pivotal role in keeping iron concentrations within a narrow physiological range in humans. The opportunity to reduce matriptase‐2 proteolytic activity may open a novel possibility to treat iron overload diseases, such as hereditary hemochromatosis and thalassemia. Here, we present 23 new analogues of trypsin inhibitor SFTI‐1 designed to inhibit human matriptase‐2. Influence of the modifications Gly1Lys, Ile10Arg, and Phe12His, as well as the introduction of Narg in P1 or P1 and P4 positions were examined. Selected peptides were further analyzed, together with previously reported peptides, for their inhibitory activity against related human proteases, that are, matriptase‐1, plasmin, thrombin and trypsin. A highly potent inhibitor of matriptase‐2, the bicycylic [Arg 5 , Arg 10 , His 12 ]SFTI‐1, with a K i value of 15 n m was obtained. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| DOI: | 10.1002/bip.23031 |
| الاتاحة: | http://dx.doi.org/10.1002/bip.23031 https://api.wiley.com/onlinelibrary/tdm/v1/articles/10.1002%2Fbip.23031 https://onlinelibrary.wiley.com/doi/pdf/10.1002/bip.23031 |
| Rights: | http://onlinelibrary.wiley.com/termsAndConditions#vor |
| رقم الانضمام: | edsbas.B7193769 |
| قاعدة البيانات: | BASE |
| DOI: | 10.1002/bip.23031 |
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