title: [Cellular test systems for the search for transcription factor activity modulators].
abstract: Test systems for monitoring activities and the search for substances activating or inhibiting transcription factors as biotargets have been designed on the basis of luciferase constructs containing binding sites for transcription factors CREB, NFAT, NF-kB, p53, STAT1, GAS, VDR, HSF1, and HIF1alpha. An assessment of the functional activity of reporter constructs has been carried out using their transient transfection into HEK293 cells followed by treatment with specific inducers. The functional activity of all reporter constructs was observed based on the increased luciferase expression. In order to evaluate the efficiency of the suggested test systems, aspirin was used. Incubation of cells transfected with the above-mentioned constructs treated with aspirin was accompanied by the suppression of NF-kB, HIF1alpha, GAS, VDR, and HSF binding activity. The findings revealed for NF-kB, NFAT, and STAT1 confirm the published data concerning the mechanisms of aspirin action. The detected effects of this drug on the HIF1alpha, GAS, VDR, and CREB activity have been demonstrated for the first time.
authors.forename: M Kh
authors.initials: MKh
authors.lastname: Salimgareeva
authors.forename: S V
authors.initials: SV
authors.lastname: Sadovnikov
authors.forename: E I
authors.initials: EI
authors.lastname: Farafontova
authors.forename: L F
authors.initials: LF
authors.lastname: Zaĭnullina
authors.forename: V A
authors.initials: VA
authors.lastname: Vakhitov
authors.forename: Iu V
authors.initials: IuV
authors.lastname: Vakhitova
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D001241:Aspirin / Q000494:pharmacology*; D001665:Binding Sites; D001681:Biological Assay; D005786:Gene Expression Regulation / Q000187:drug effects*; D017930:Genes, Reporter; D057809:HEK293 Cells; D006801:Humans; D008156:Luciferases / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D011401:Promoter Regions, Genetic; D014157:Transcription Factors / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D014158:Transcription, Genetic / Q000187:drug effects*; D014162:Transfection
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D014157:Transcription Factors; D008156:Luciferases; D001241:Aspirin