New Peptolides from the CyanobacteriumNostoc insulareas Selective and Potent Inhibitors of Human Leukocyte Elastase
| Autor: | Stefan Kehraus, Gabriele M. König, Christian Mehner, Daniela Müller, Stephanie Hautmann, Michael Gütschow |
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| Rok vydání: | 2008 |
| Předmět: |
Cyanobacteria
Cathepsin G Magnetic Resonance Spectroscopy Myeloblastin Peptides Cyclic Biochemistry Substrate Specificity Human Leukocyte Elastase Inhibitory Concentration 50 Drug Discovery Humans Amino Acid Sequence Enzyme Inhibitors Nostoc Molecular Biology IC50 chemistry.chemical_classification biology Serine Endopeptidases Organic Chemistry biology.organism_classification Cathepsins Enzyme chemistry Molecular Medicine Cyanobacterium nostoc Biological Assay Leukocyte Elastase |
| Zdroj: | ChemBioChem. 9:2692-2703 |
| ISSN: | 1439-7633 1439-4227 |
| DOI: | 10.1002/cbic.200800415 |
| Popis: | Eight new cyanopeptolins (insulapeptolides A-H) were obtained from the cyanobacterium Nostoc insulare. Their isolation was guided by their bioactivity toward the target enzyme human leukocyte elastase, molecular biological investigations, and MALDI-TOF analysis. These peptides are selective inhibitors of human leukocyte elastase with activities in the nanomolar range. Insulapeptolide D was the most potent compound with an IC(50) value of 85 nM (K(i) value of 36 nM). |
| Databáze: | OpenAIRE |
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