6533b85afe1ef96bd12b8bdc

RESEARCH PRODUCT

1-ethyl-3-(6-methylphenanthridine-8-il) urea modulates TLR3/9 activation and induces selective pro-inflammatory cytokine expression in vitro.

Marijana Radić StojkovićAdriana LepurAlexander N.r. WeberIvo PiantanidaKatja EsterMahjoub BihiOliver VugrekDamir VrbanecNatalija Knežević TeofilovićDragomira MajhenZlatko DembicAlemka MarkotićMustafa DikenMarijeta KraljNada OršolićJelena KneževićLidija Tumir

subject

0301 basic medicineClinical BiochemistryPharmaceutical ScienceDown-RegulationBiochemistryCell Line03 medical and health sciences0302 clinical medicineImmune systemDrug DiscoveryHumansImmunologic FactorsUreaSecretionReceptorMolecular BiologyInnate immune systemChemistryInterleukin-6Tumor Necrosis Factor-alphaOrganic ChemistryInterleukin-8Interferon-alphaTLR7Molecular biologyphenantridines ; TLR ; PBMCs ; cytokines ; immunomodulationIntercalating AgentsPhenanthridinesToll-Like Receptor 3030104 developmental biologyOligodeoxyribonucleotidesToll-Like Receptor 9TLR3Nucleic acidMolecular MedicineTumor necrosis factor alpha030215 immunologySignal Transduction

description

We have previously demonstrated the nucleic acid binding capacity of phenanthridine derivatives (PHTs). Because nucleic acids are potent inducers of innate immune response through Toll-like receptors (TLRs), and because PTHs bear a structural resemblance to commonly used synthetic ligands for TLR7/8, we hypothesized that PHTs could modulate/activate immune response. We found that compound M199 induces secretion of IL-6, IL-8 and TNFα in human PBMCs and inhibits TLR3/9 activation in different cellular systems (PBMCs, HEK293 and THP-1 cell lines).

yearjournalcountryeditionlanguage
2017-04-01Bioorganicmedicinal chemistry letters
10.1016/j.bmcl.2017.02.048https://pubmed.ncbi.nlm.nih.gov/28254484