User: Guest  Login
Less Searchfields
Simple search
Title:

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

Document type:
Article; Journal Article
Author(s):
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...     »
Journal title abbreviation:
Eur J Med Chem
Year:
2022
Journal volume:
238
Fulltext / DOI:
doi:10.1016/j.ejmech.2022.114437
Pubmed ID:
http://view.ncbi.nlm.nih.gov/pubmed/35635944
Print-ISSN:
0223-5234
TUM Institution:
Klinik und Poliklinik für Frauenheilkunde
 BibTeX