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Titel:

Improving the selectivity of 3-amidinophenylalanine-derived matriptase inhibitors.

Dokumenttyp:
Article; Journal Article
Autor(en):
Pilgram, Oliver; Keils, Aline; Benary, Gerrit E; Müller, Janis; Merkl, Stefan; Ngaha, Sandrine; Huber, Simon; Chevillard, Florent; Harbig, Anne; Magdolen, Viktor; Heine, Andreas; Böttcher-Friebertshäuser, Eva; Steinmetzer, Torsten
Abstract:
A rational structure-based approach was employed to develop novel 3-amidinophenylalanine-derived matriptase inhibitors with improved selectivity against thrombin and factor Xa. Of all 23 new derivatives, several monobasic inhibitors exhibit high matriptase affinities and strong selectivity against thrombin. Some inhibitors also possess selectivity against factor Xa, although less pronounced as found for thrombin. A crystal structure of a selective monobasic matriptase inhibitor in complex with m...     »
Zeitschriftentitel:
Eur J Med Chem
Jahr:
2022
Band / Volume:
238
Volltext / DOI:
doi:10.1016/j.ejmech.2022.114437
PubMed:
http://view.ncbi.nlm.nih.gov/pubmed/35635944
Print-ISSN:
0223-5234
TUM Einrichtung:
Klinik und Poliklinik für Frauenheilkunde
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