Journal
CHEMBIOCHEM
Volume 18, Issue 10, Pages 888-893Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.201600650
Keywords
inhibitors; NETosis; neutrophil extracellular traps (NETs); structure-activity relationships; tetrahydroisoquinolines
Funding
- IMPRS Chemical Biology Program
- MPG
- Fonds der Chemischen Industrie
- European Research Council under the European Union [268309]
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Neutrophils are short-lived leukocytes that migrate to sites of infection as part of the acute immune response, where they phagocytose, degranulate, and form neutrophil extracellular traps (NETs). During NET formation, the nuclear lobules of neutrophils disappear and the chromatin expands and, accessorized with neutrophilic granule proteins, is expelled. NETs can be pathogenic in, for example, sepsis, cancer, and autoimmune and cardiovascular diseases. Therefore, the identification of inhibitors of NET formation is of great interest. Screening of a focused library of natural-product-inspired compounds by using a previously validated phenotypic NET assay identified a group of tetrahydroisoquinolines as new NET formation inhibitors. This compound class opens up new avenues for the study of cellular death through NET formation (NETosis) at different stages, and might inspire new medicinal chemistry programs aimed at NET-dependent diseases.
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