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ID: ALA4007458

Journal: Bioorg Med Chem Lett

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

Authors: Teofilović NK, Bihi M, Stojković MR, Tumir LM, Ester K, Kralj M, Majhen D, Oršolić N, Lepur A, Vrbanec D, Markotić A, Dembić Z, Weber AN, Piantanida I, Vugrek O, Diken M, Knežević J.

Abstract: 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).

CiteXplore: 28254484

DOI: 10.1016/j.bmcl.2017.02.048