Substituted flavones as aryl hydrocarbon (Ah) receptor agonists and antagonists

Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

1973 • 12,522 citations

2,3,7,8-Tetrachlorodibenzo-p-Dioxin and Related Halogenated Aromatic Hydrocarbons: Examination of the Mechanism of Toxicity

1982 • 2,512 citations

Polychlorinated Biphenyls (PCBs), Dibenzo-p-Dioxins (PCDDs), Dibenzofurans (PCDFs), and Related Compounds: Environmental and Mechanistic Considerations Which Support the Development of Toxic Equivalency Factors (TEFs)

1990 • 1,872 citations

Induction of microsomal enzymes by foreign chemicals and carcinogenesis by polycyclic aromatic hydrocarbons: G. H. A. Clowes Memorial Lecture.

1982 • 1,559 citations

Stereospecific, high affinity binding of 2,3,7,8-tetrachlorodibenzo-p-dioxin by hepatic cytosol. Evidence that the binding species is receptor for induction of aryl hydrocarbon hydroxylase.

1976 • 1,343 citations

Cloning of a Factor Required for Activity of the Ah (Dioxin) Receptor

1991 • 963 citations

Cloning of the Ah-receptor cDNA reveals a distinctive ligand-activated transcription factor.

1992 • 830 citations

A rapid method for assaying the metabolism of 7-ethoxyresorufin by microsomal subcellular fractions

1980 • 827 citations

Comparative Toxicology and Mechanism of Action of Polychlorinated Dibenzo-P-Dioxins and Dibenzofurans

1986 • 707 citations

The DNA recognition site for the dioxin-Ah receptor complex. Nucleotide sequence and functional analysis.

1988 • 455 citations

cDNA cloning and structure of mouse putative Ah receptor

1992 • 406 citations

Regulatory gene product of the Ah locus. Characterization of the cytosolic inducer-receptor complex and evidence for its nuclear translocation.

1979 • 401 citations

The Ah receptor: Mediator of the toxicity of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and related compounds☆

1994 • 380 citations

Mechanistic aspects of dioxin action

1993 • 372 citations

Modulation of gene expression and endocrine response pathways by 2,3,7,8-tetrachlorodibenzo-p-dioxin and related compounds

1995 • 369 citations

Cloning and expression of a human Ah receptor cDNA.

1993 • 334 citations

Dioxin binding activities of polymorphic forms of mouse and human arylhydrocarbon receptors.

1994 • 327 citations

Protein-DNA Interactions at Recognition Sites for the Dioxin-Ah Receptor Complex

1989 • 215 citations

Biological Basis for Risk Assessment of Dioxins and Related Compounds

1991 • 212 citations

Ah receptor binding properties of indole carbinols and induction of hepatic estradiol hydroxylation

1993 • 190 citations

The Ah locus: Correlation of intranuclear appearance of inducer-receptor complex with induction of cytochrome P1-450 mRNA

1982 • 184 citations

The examination and quantitation of tissue cytosolic receptors for 2,3,7,8-tetrachlorodibenzo-p-dioxin using hydroxylapatite

1982 • 168 citations

Ah receptor in human placenta: stabilization by molybdate and characterization of binding of 2,3,7,8-tetrachlorodibenzo-p-dioxin, 3-methylcholanthrene, and benzo(a)pyrene.

1987 • 167 citations

Mechanism of action and structure-activity relationships for the chlorinated dibenzo-p-dioxins and related compounds

1989 • 154 citations

Interactions of indoles with specific binding sites for 2,3,7,8-tetrachlorodibenzo-p-dioxin in rat liver.

1985 • 145 citations

Molecular characterization of the murine Ahr gene. Organization, promoter analysis, and chromosomal assignment.

1993 • 141 citations

Alpha-naphthoflavone acts as an antagonist of 2,3,7, 8-tetrachlorodibenzo-p-dioxin by forming an inactive complex with the Ah receptor.

1991 • 136 citations

Specificity in the activation and inhibition by flavonoids of benzo[a]pyrene hydroxylation by cytochrome P-450 isozymes from rabbit liver microsomes.

1981 • 119 citations

Identification of 3′-Methoxy-4′-nitroflavone as a Pure Aryl Hydrocarbon (Ah) Receptor Antagonist and Evidence for More Than One Form of the Nuclear Ah Receptor in MCF-7 Human Breast Cancer Cells

1995 • 108 citations

Variation in the molecular mass of the Ah receptor among vertebrate species and strains of rats

1987 • 108 citations

Interactions of indolo[3,2-b]carbazoles and related polycyclic aromatic hydrocarbons with specific binding sites for 2,3,7,8-tetrachlorodibenzo-p-dioxin in rat liver.

1993 • 100 citations

2,3,7,8-Tetrachlorodibenzo-p-dioxin versus 3-methylcholanthrene: comparative studies of Ah receptor binding, transformation, and induction of CYP1A1.

1994 • 97 citations

Mechanism of Action of α-Naphthoflavone as an Ah Receptor Antagonist in MCF-7 Human Breast Cancer Cells

1993 • 92 citations

alpha-Naphthoflavone-induced CYP1A1 gene expression and cytosolic aryl hydrocarbon receptor transformation.

1993 • 88 citations

Effects of structure on binding to the 2,3,7,8-TCDD receptor protein and AHH induction--halogenated biphenyls.

1985 • 85 citations

Mechanism of action of aryl hydrocarbon receptor antagonists: Inhibition of 2,3,7,8-tetrachlorodibenzo-p-dioxin-induced CYP1A1 gene expression

1992 • 69 citations

Halogenated biphenyls, terphenyls, naphthalenes, dibenzodioxins and related compounds

1982 • 66 citations

Competitive binding to the cytosolic 2,3,7,8-tetrachlorodibenzo-p-dioxin receptor

1983 • 62 citations

Synthesis and biological evaluation of a series of flavones designed as inhibitors of protein tyrosine kinases.

1992 • 62 citations

Partial antagonism of 2,3,7,8-tetrachlorodibenzo-p-dioxin-mediated induction of aryl hydrocarbon hydroxylase by 6-methyl-1,3,8-trichlorodibenzofuran: mechanistic studies.

1989 • 58 citations

Role of the ligand in intracellular receptor function: receptor affinity determines activation in vitro of the latent dioxin receptor to a DNA-binding form.

1991 • 51 citations

Effects of Structure on Binding to the 2,3,7,8-TCDD Receptor Protein and AHH Induction. Halogenated Biphenyls

1985 • 46 citations

Effects of substituents on the cytosolic receptor-binding avidities and aryl hydrocarbon hydroxylase induction potencies of 7-substituted 2,3-dichlorodibenzo-p-dioxins. A quantitative structure-activity relationship analysis.

1985 • 40 citations

Quantitative structure-activity relationships: analysis of interactions of 2,3,7,8-tetrachlorodibenzo-p-dioxin and 2-substituted analogues with rat, mouse, guinea pig, and hamster cytosolic receptor.

1987 • 35 citations

Binding characteristics of Ah receptors from rats and mice before and after separation from hepatic cytosols

1988 • 32 citations

Induction of cytochrome P450-dependent monooxygenase activities in rat hepatoma H-4-IIE cells in culture by 2,3,7,8-tetrachlorodibenzo-p-dioxin and related compounds: Mechanistic studies using radiolabeled congeners

1989 • 30 citations

Substituted polychlorinated dibenzofuran receptor binding affinites and aryl hydrocarbon hydroxylase induction potencies — A QSAR analysis

1986 • 29 citations

Chelatable metal ions are not required for aryl hydrocarbon receptor transformation to a DNA binding form: Phenanthrolines are possible competitive antagonists of 2,3,7,8-tetrachlorodibenzo-p-dioxin

1992 • 22 citations

Characterization of an inducible aryl hydrocarbon receptor-like protein in rat liver

1991 • 21 citations

6-Substituted 3,4-Benzocoumarins: A New Structural Class of Inducers and Inhibitors of CYP1A1-Dependent Activity

1993 • 19 citations

Evidence for two functionally distinct forms of the human Ah receptor

1995 • 16 citations

2-Phenylphenanthridinone and Related Compounds: Aryl Hydrocarbon Receptor Agonists and Suicide Inactivators of P4501A1

1994 • 13 citations

Effect of Ligand Structure on Formation and DNA Binding Properties of the Transformed Rat Cytosolic Aryl Hydrocarbon Receptor

1994 • 12 citations

Inhibition of hepatic aryl hydrocarbon hydroxylase by 3-methylcholanthrene, 7,8-benzoflavone and other inducers added in vitro

1975 • 12 citations

Heterogeneity of rat hepatic Ah Receptor: Identification of two receptor forms which differ in their biochemical properties

1992 • 10 citations

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