Matches in SemOpenAlex for { <https://semopenalex.org/work/W1931584318> ?p ?o ?g. }
Showing items 1 to 64 of
64
with 100 items per page.
- W1931584318 abstract "Mepacrine has been used for decades and the beneficial effects of this drug are well described. Since endothelial cells (EC) are in many cases the first cells to come in contact with drugs, the effect of mepacrine on certain aspects of EC biology were studied. First, our data demonstrate that at high doses mepacrine can have a marked impact on the integrity of the EC monolayer without grossly interfering with cell viability. The described impact of mepacrine on EC might explain, at least in part, the negative effects of this drug observed in the past. More importantly, mepacrine profoundly effects gene regulation in EC and fibroblasts. Mepacrine binds to DNA in a sequence specific manner. While NF-kB-DNA interactions are not effected, AP-1-DNA binding is blocked by mepacrine. Such differential effects are presumably due to sequence specific intercalation of mepacrine into the AP-1 consensus element. Pre-incubation of oligonucleotides resembling this sequence blocked the subsequent binding of nuclear extract containing AP-1 protein(s). Consequently, mepacrine prevents the upregulation of genes which depend mainly on the activation of AP-1. One of the few genes which have been found to depend heavily on the activation of this transcription factor is metalloproteinase-1 (MMP-1). We demonstrated by western blot that treatment of fibroblasts with mepacrine completely prevented subsequent upregulation of MMP-1. Since MMP-1 plays an important role in the propagation of rheumatic diseases, we suggest that the beneficial effect of mepacrine seen in the past is due, at least in part, to the described mechanisms." @default.
- W1931584318 created "2016-06-24" @default.
- W1931584318 creator A5043255698 @default.
- W1931584318 creator A5044141373 @default.
- W1931584318 creator A5069754389 @default.
- W1931584318 date "2001-01-26" @default.
- W1931584318 modified "2023-10-04" @default.
- W1931584318 title "Specific suppression of the transcription factor AP-1 by mepacrine" @default.
- W1931584318 cites W2172078816 @default.
- W1931584318 doi "https://doi.org/10.1186/ar213" @default.
- W1931584318 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3273180" @default.
- W1931584318 hasPublicationYear "2001" @default.
- W1931584318 type Work @default.
- W1931584318 sameAs 1931584318 @default.
- W1931584318 citedByCount "0" @default.
- W1931584318 crossrefType "journal-article" @default.
- W1931584318 hasAuthorship W1931584318A5043255698 @default.
- W1931584318 hasAuthorship W1931584318A5044141373 @default.
- W1931584318 hasAuthorship W1931584318A5069754389 @default.
- W1931584318 hasBestOaLocation W19315843181 @default.
- W1931584318 hasConcept C104317684 @default.
- W1931584318 hasConcept C126322002 @default.
- W1931584318 hasConcept C198451711 @default.
- W1931584318 hasConcept C203014093 @default.
- W1931584318 hasConcept C2778048844 @default.
- W1931584318 hasConcept C2779291727 @default.
- W1931584318 hasConcept C2991849723 @default.
- W1931584318 hasConcept C54355233 @default.
- W1931584318 hasConcept C71924100 @default.
- W1931584318 hasConcept C86339819 @default.
- W1931584318 hasConcept C86803240 @default.
- W1931584318 hasConcept C95444343 @default.
- W1931584318 hasConceptScore W1931584318C104317684 @default.
- W1931584318 hasConceptScore W1931584318C126322002 @default.
- W1931584318 hasConceptScore W1931584318C198451711 @default.
- W1931584318 hasConceptScore W1931584318C203014093 @default.
- W1931584318 hasConceptScore W1931584318C2778048844 @default.
- W1931584318 hasConceptScore W1931584318C2779291727 @default.
- W1931584318 hasConceptScore W1931584318C2991849723 @default.
- W1931584318 hasConceptScore W1931584318C54355233 @default.
- W1931584318 hasConceptScore W1931584318C71924100 @default.
- W1931584318 hasConceptScore W1931584318C86339819 @default.
- W1931584318 hasConceptScore W1931584318C86803240 @default.
- W1931584318 hasConceptScore W1931584318C95444343 @default.
- W1931584318 hasIssue "S2" @default.
- W1931584318 hasLocation W19315843181 @default.
- W1931584318 hasLocation W19315843182 @default.
- W1931584318 hasOpenAccess W1931584318 @default.
- W1931584318 hasPrimaryLocation W19315843181 @default.
- W1931584318 hasRelatedWork W1931584318 @default.
- W1931584318 hasRelatedWork W1975595193 @default.
- W1931584318 hasRelatedWork W2003523972 @default.
- W1931584318 hasRelatedWork W2057841153 @default.
- W1931584318 hasRelatedWork W2110646266 @default.
- W1931584318 hasRelatedWork W2622204852 @default.
- W1931584318 hasRelatedWork W2949283095 @default.
- W1931584318 hasRelatedWork W4254747857 @default.
- W1931584318 hasRelatedWork W4255039225 @default.
- W1931584318 hasRelatedWork W4367397467 @default.
- W1931584318 hasVolume "3" @default.
- W1931584318 isParatext "false" @default.
- W1931584318 isRetracted "false" @default.
- W1931584318 magId "1931584318" @default.
- W1931584318 workType "article" @default.