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Image Search Results
Journal: Chemmedchem
Article Title: Biological Characterization, Mechanistic Investigation and Structure‐Activity Relationships of Chemically Stable TLR2 Antagonists
doi: 10.1002/cmdc.202000060
Figure Lengend Snippet: Inhibition of TLR2‐dependent NF‐κB activation and IL‐8 secretion. A) HEK‐Blue hTLR2 cells were pre‐incubated with CU‐CPT22 or compounds 1 – 6 and 9 – 11 for 1 h and then stimulated additionally with TLR2/1 agonist Pam 3 CSK 4 (10 ng/mL) or TLR2/6 agonist Pam 2 CSK 4 (1 ng/mL) for 24 h. B) HEK‐Blue hTLR2 cells were pre‐incubated with increasing concentrations of 4 , 6 , 9 , 10 and then stimulated additionally with Pam 3 CSK 4 or Pam 2 CSK 4 for 24 h. Supernatants were tested for TLR2‐mediated NF‐κB/AP‐1 activity by quantification of SEAP release (OD 640 ). C) THP‐1 macrophages were incubated with CU‐CPT22 (25 μM) or compound 6 for 1 h and afterwards stimulated with Pam 3 CSK 4 (10 ng/mL), Pam 2 CSK 4 (1ng/mL), LPS (10 ng/mL), flagellin (1 μg/mL), CL075 (8 μM) or ODN2006 (5 μM) for 24 h. Supernatants were analyzed for IL‐8 secretion by ELISA. Mean+SD or ±SD ( n =3).
Article Snippet: TLR2 ligands : The synthetic lipopeptides Pam 3 CSK 4 and Pam 2 CSK 4 , lipopolysaccharide from Escherichia coli O111:B4 (LPS‐EB), flagellin from Salmonella typhimurium (FLA‐ST), the thiazoloquinoline compound CL075 and
Techniques: Inhibition, Activation Assay, Incubation, Activity Assay, Enzyme-linked Immunosorbent Assay