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Selective high affinity retinoic acid receptor alpha or beta-gamma ligands.
TLDR
Two complementary assays are set up, an in vitro binding assay to determine the Kd values of retinoids for RAR alpha, RAR beta, and RAR gamma and a functional assay in cultured cells to evaluate the potential of Retinoids to transactivate, through their binding to one type of RAR, a reporter gene. Expand
Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma.
TLDR
Using in vitro binding studies and a functional transactivation assay, this work has identified three compounds with high RAR gamma selectivity that could provide therapeutic entities with a higher therapeutic index at lower teratogenic risk. Expand
Is CYP1A1 induction always related to AHR signaling pathway?
TLDR
Results from the literature indicate that induction of CYP1A1 does not only involve the classical activation cascade of the Ah receptor, but also includes other signaling pathways, including the RARs signal transduction pathway, as already described for retinoic acid. Expand
The role of protein tyrosine kinases in CYP1A1 induction by omeprazole and thiabendazole in rat hepatocytes.
TLDR
Results are consistent with the implication of a tyrosine kinase, most probably the Src tyrosinesine Kinase, in the mechanism of CYP1A1 induction in rat hepatocytes. Expand
Cytochrome 1A1 induction by primaquine in human hepatocytes and HepG2 cells: absence of binding to the aryl hydrocarbon receptor.
TLDR
Data suggest that CYP1A1 induction involves the participation of the AhR but not a direct primaquine-receptor interaction, which supports the notion that an alternative ligand-independent mechanism has to be considered in the treatment of malaria. Expand
Induction of cytochrome P450 1A1 gene expression, oxidative stress, and genotoxicity by carbaryl and thiabendazole in transfected human HepG2 and lymphoblastoid cells.
TLDR
Observations support the notion that intracellular signals leading to CYP1A1 induction, oxidative stress, and genotoxicity are intimately related, as demonstrated by the dose-dependent increase in reporter CAT and CYP 1A1 mRNAs. Expand
Carbaryl induces CYP1A1 gene expression in HepG2 and HaCaT cells but is not a ligand of the human hepatic Ah receptor.
TLDR
Data suggest that induction of CYP1A1 involves the participation of the AhR and the XRE, but is not mediated by a direct carbaryl-receptor interaction, and an alternative ligand-independent mechanism should be considered. Expand
Cytotoxic effects and induction of cytochromes P450 1A1/2 by insecticides, in hepatic or epidermal cells: binding capability to the Ah receptor.
TLDR
Except for cypermethrin and diflubenzuron, all these chemicals exerted a cytotoxic effect in hepatocytes and HaCaT, but not in HepG2 cells, suggesting that they would not be a ligand of the Ah receptor. Expand
Diflubenzuron, a benzoyl-urea insecticide, is a potent inhibitor of TCDD-induced CYP1A1 expression in HepG2 cells.
TLDR
Results support the involvement of a transcriptional mechanism in the inhibition of CYP1A1 expression in HepG2 cells by DFB, possibly via an Ah receptor antagonism. Expand
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