title: 1-[4-Fluoro-2-(2-nitrovinyl)phenyl]pyrrolidine Suppresses Toll-Like Receptor 4 Dimerization Induced by Lipopolysaccharide.
abstract: Toll-like receptor 4 (TLR4) recognizes LPS and triggers the activation of the myeloid differential factor 88 (MyD88)- and toll-interleukin-1 receptor domain-containing adapter, inducing interferon-β (TRIF)-dependent major downstream signaling pathways. Previously, we presented biochemical evidence that 1-[4-Fluoro-2-(2-nitrovinyl)phenyl]pyrrolidine (FPP), which was synthesized in our laboratory, inhibits NF-κB activation induced by LPS. Here, we investigated whether FPP modulates the TLR4 downstream signaling pathways and what anti-inflammatory target in TLR4 signaling is regulated by FPP. FPP inhibited LPS-induced NF-κB activation by targeting TLR4 dimerization. These results suggest that FPP can modulate the TLR4 signaling pathway at the receptor level to decrease inflammatory gene expression.
authors.affiliation: a Department of Medical Science , College of Medical Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.
authors.forename: Sang-Ii
authors.initials: SI
authors.lastname: Ahn
authors.affiliation: a Department of Medical Science , College of Medical Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.
authors.forename: Ji-Soo
authors.initials: JS
authors.lastname: Kim
authors.affiliation: b Department of Biomedical Laboratory Science , College of Medical Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.
authors.forename: Chae-Yeon
authors.initials: CY
authors.lastname: Hong
authors.affiliation: a Department of Medical Science , College of Medical Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.
authors.forename: Gyo-Jeong
authors.initials: GJ
authors.lastname: Gu
authors.affiliation: b Department of Biomedical Laboratory Science , College of Medical Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.
authors.forename: Hyeon-Myeong
authors.initials: HM
authors.lastname: Shin
authors.affiliation: c Department of Chemistry , College of Natural Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.
authors.forename: Hyun Jung
authors.initials: HJ
authors.lastname: Jeong
authors.affiliation: c Department of Chemistry , College of Natural Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.
authors.forename: Kwang Oh
authors.initials: KO
authors.lastname: Koh
authors.affiliation: c Department of Chemistry , College of Natural Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.
authors.forename: Joo Yang
authors.initials: JY
authors.lastname: Mang
authors.affiliation: c Department of Chemistry , College of Natural Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.
authors.forename: Dae Young
authors.initials: DY
authors.lastname: Kim
authors.affiliation: a Department of Medical Science , College of Medical Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.|b Department of Biomedical Laboratory Science , College of Medical Sciences, SoonChunHyang University , Asan-Si , Chungnam , Republic of Korea.
authors.forename: Hyung-Sun
authors.initials: HS
authors.lastname: Youn
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D057809:HEK293 Cells; D006801:Humans; D008070:Lipopolysaccharides / Q000494:pharmacology*; D051379:Mice; D015394:Molecular Structure; D016328:NF-kappa B / Q000378:metabolism; D011485:Protein Binding / Q000187:drug effects; D055503:Protein Multimerization / Q000187:drug effects*; D011759:Pyrrolidines / Q000494:pharmacology*; D051197:Toll-Like Receptor 4 / Q000737:chemistry / Q000378:metabolism*; D014753:Vinyl Compounds / Q000494:pharmacology*
chemical_list: C000601182:1-(4-fluoro-2-(2-nitrovinyl)phenyl)pyrrolidine; D008070:Lipopolysaccharides; D016328:NF-kappa B; D011759:Pyrrolidines; C495345:TLR4 protein, human; C493487:Tlr4 protein, mouse; D051197:Toll-Like Receptor 4; D014753:Vinyl Compounds
keywords: 1-[4-Fluoro-2-(2-nitrovinyl)phenyl]pyrrolidine; NF-κB; dimerization; inflammation; lipopolysaccharide; toll-like receptor 4