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• W3129095941 endingPage "100353" @default.
• W3129095941 startingPage "100353" @default.
• W3129095941 abstract "Polychlorinated bisphenols (PCBs) continue to contaminate food chains globally where they concentrate in tissues and disrupt the endocrine systems of species throughout the ecosphere. Hydroxylated PCBs (OH-PCBs) are major PCB metabolites and high-affinity inhibitors of human estrogen sulfotransferase (SULT1E1), which sulfonates estrogens and thus prevents them from binding to and activating their receptors. OH-PCB inhibition of SULT1E1 is believed to contribute significantly to PCB-based endocrine disruption. Here, for the first time, the molecular basis of OH-PCB inhibition of SULT1E1 is revealed in a structure of SULT1E1 in complex with OH-PCB1 (4ʹ-OH-2,6-dichlorobiphenol) and its substrates, estradiol (E2), and PAP (3'-phosphoadenosine-5-phosphosulfate). OH-PCB1 prevents catalysis by intercalating between E2 and catalytic residues and establishes a new E2-binding site whose E2 affinity and positioning are greater than and competitive with those of the reactive-binding pocket. Such complexes have not been observed previously and offer a novel template for the design of high-affinity inhibitors. Mutating residues in direct contact with OH-PCB weaken its affinity without compromising the enzyme's catalytic parameters. These OH-PCB resistant mutants were used in stable transfectant studies to demonstrate that OH-PCBs regulate estrogen receptors in cultured human cell lines by binding the OH-PCB binding pocket of SULT1E1." @default.
• W3129095941 created "2021-02-15" @default.
• W3129095941 creator A5002116715 @default.
• W3129095941 creator A5068080767 @default.
• W3129095941 creator A5073390440 @default.
• W3129095941 date "2021-01-01" @default.
• W3129095941 modified "2023-10-12" @default.
• W3129095941 title "The molecular basis of OH-PCB estrogen receptor activation" @default.
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• W3129095941 doi "https://doi.org/10.1016/j.jbc.2021.100353" @default.
• W3129095941 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7949139" @default.
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• W3129095941 hasPublicationYear "2021" @default.
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