Tetrahydroisoquinolines: New Inhibitors of Neutrophil Extracellular Trap (NET) Formation.
Chembiochem
; 18(10): 888-893, 2017 05 18.
Article
em En
| MEDLINE
| ID: mdl-28240414
ABSTRACT
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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tetra-Hidroisoquinolinas
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Armadilhas Extracelulares
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Lúpus Eritematoso Sistêmico
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Neutrófilos
Limite:
Humans
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article