Mebendazole-induced M1 polarisation of THP-1 macrophages may involve DYRK1B inhibition.
Antigens, CD
/ genetics
Antigens, Differentiation, Myelomonocytic
/ genetics
Antinematodal Agents
/ metabolism
Cell Differentiation
/ drug effects
Gene Expression Regulation
Heterocyclic Compounds, 2-Ring
/ pharmacology
Humans
Interferon-gamma
/ genetics
Interleukins
/ genetics
Lipopolysaccharides
/ pharmacology
Macrophages
/ cytology
Mebendazole
/ metabolism
Phosphorylation
/ drug effects
Protein Binding
Protein Kinase Inhibitors
/ pharmacology
Protein Serine-Threonine Kinases
/ antagonists & inhibitors
Protein-Tyrosine Kinases
/ antagonists & inhibitors
Proto-Oncogene Proteins c-abl
/ genetics
Pyrimidines
/ pharmacology
Receptors, Cell Surface
/ genetics
Signal Transduction
THP-1 Cells
Tetradecanoylphorbol Acetate
/ pharmacology
Dyrk Kinases
DYRK1B
M1 polarisation
Mebendazole
Monocytes and macrophages
Journal
BMC research notes
ISSN: 1756-0500
Titre abrégé: BMC Res Notes
Pays: England
ID NLM: 101462768
Informations de publication
Date de publication:
22 Apr 2019
22 Apr 2019
Historique:
received:
09
01
2019
accepted:
15
04
2019
entrez:
24
4
2019
pubmed:
24
4
2019
medline:
27
8
2019
Statut:
epublish
Résumé
We recently showed that the anti-helminthic compound mebendazole (MBZ) has immunomodulating activity by inducing a M2 to M1 phenotype switch in monocyte/macrophage models. In the present study we investigated the potential role of protein kinases in mediating this effect. MBZ potently binds and inhibits Dual specificity tyrosine-phosphorylation-regulated kinase 1B (DYRK1B) with a Kd and an IC
Identifiants
pubmed: 31010428
doi: 10.1186/s13104-019-4273-5
pii: 10.1186/s13104-019-4273-5
pmc: PMC6477744
doi:
Substances chimiques
AZ191 compound
0
Antigens, CD
0
Antigens, Differentiation, Myelomonocytic
0
Antinematodal Agents
0
CD163 antigen
0
Heterocyclic Compounds, 2-Ring
0
Interleukins
0
Lipopolysaccharides
0
Protein Kinase Inhibitors
0
Pyrimidines
0
Receptors, Cell Surface
0
Mebendazole
81G6I5V05I
Interferon-gamma
82115-62-6
Protein-Tyrosine Kinases
EC 2.7.10.1
ABL1 protein, human
EC 2.7.10.2
Proto-Oncogene Proteins c-abl
EC 2.7.10.2
Protein Serine-Threonine Kinases
EC 2.7.11.1
Tetradecanoylphorbol Acetate
NI40JAQ945
Types de publication
Journal Article
Langues
eng
Pagination
234Subventions
Organisme : Cancerfonden
ID : Can 2016/335
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