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Tetrahydroisoquinolines: New Inhibitors of Neutrophil Extracellular Trap (NET) Formation
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2017 (English)In: ChemBioChem (Print), ISSN 1439-4227, E-ISSN 1439-7633, Vol. 18, no 10, 888-893 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
Wiley-VCH Verlagsgesellschaft, 2017. Vol. 18, no 10, 888-893 p.
Keyword [en]
inhibitors, NETosis, neutrophil extracellular traps (NETs), structure-activity relationships, trahydroisoquinolines
National Category
Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)
Identifiers
URN: urn:nbn:se:umu:diva-135969DOI: 10.1002/cbic.201600650ISI: 000401868700004PubMedID: 28240414OAI: oai:DiVA.org:umu-135969DiVA: diva2:1115632
Available from: 2017-06-27 Created: 2017-06-27 Last updated: 2017-06-27Bibliographically approved

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Hedberg, Christian
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Department of ChemistryUmeå Centre for Microbial Research (UCMR)
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CiteExportLink to record
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Cite
Citation style
  • apa
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  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
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  • en-US
  • fi-FI
  • nn-NO
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