Refine
Has Fulltext
- yes (22)
Is part of the Bibliography
- yes (22)
Year of publication
Document Type
- Journal article (22)
Language
- English (22)
Keywords
- Biologie (5)
- actinomycetes (5)
- sponges (4)
- marine sponge (3)
- marine sponges (3)
- streptomyces (3)
- NRPS (2)
- Streptomyces (2)
- Streptomyces axinellae (2)
- anti-parasitic (2)
Institute
- Julius-von-Sachs-Institut für Biowissenschaften (21)
- Theodor-Boveri-Institut für Biowissenschaften (3)
- Institut für Pharmakologie und Toxikologie (2)
- Augenklinik und Poliklinik (1)
- Center for Computational and Theoretical Biology (1)
- Institut für Molekulare Infektionsbiologie (1)
- Institut für Organische Chemie (1)
- Institut für Pharmazie und Lebensmittelchemie (1)
EU-Project number / Contract (GA) number
- 311932 (4)
In this paper, we report new protease inhibitory activity of plakortide E towards cathepsins and cathepsin-like parasitic proteases. We further report on its anti-parasitic activity against Trypanosoma brucei with an IC50 value of 5 mu M and without cytotoxic effects against J774.1 macrophages at 100 mu M concentration. Plakortide E was isolated from the sponge Plakortis halichondroides using enzyme assay-guided fractionation and identified by NMR spectroscopy and mass spectrometry. Furthermore, enzyme kinetic studies confirmed plakortide E as a non-competitive, slowly-binding, reversible inhibitor of rhodesain.