Transforming growth factor β1 (TGFβ1) is a potent stimulator of epithelial-to-mesenchymal transition (EMT) and has been associated with chronic kidney diseases by activating profibrotic gene expression. In this study, we investigated the role of the KEAP1-NRF2 pathway, which is a master regulator of the cellular antioxidant system, in TGFβ1-stimulated EMT gene changes using human renal tubular ...

BACKGROUND The evidence of an association between the Sulfotransferase 1A1 (SULT1A1) Arg213His polymorphism (rs9282861) and bladder cancer risk is still conflicting. We conducted a meta-analysis to assess the association between this polymorphism and bladder cancer risk. MATERIAL AND METHODS PubMed, EMBASE, HuGE Navigator, and Web of Science databases were searched for correlative articles. T...

TokyoGreen (TG) derivatives were found to be efficient and specific substrates of an important drug-metabolizing enzyme, UDP-glucuronosyltransferase (UGT) 1A1. A rapid, specific, and sensitive assay of the enzyme was achieved simply by monitoring the change in fluorescence intensity. We also designed and developed the first "turn-on" fluorescent probes for UGTs.

Background: Human cytochrome P450 1A1 (CYP1A1) activates procarcinogens but the basis of their binding is unknown. Results: A 2.6 Å structure with the inhibitor αnaphthoflavone and docking simulations suggest key active site features. Conclusion: CYP1A1 has a planar active site that restricts ligand orientations. Significance: This provides a useful framework for understanding CYP1A1 interactio...

UDP-glucuronosyltransferase 1A1 (UGT1A1) is a vital metabolic enzyme responsible for the clearance of endogenous substances and drugs. Hitherto, development fluorescent probes UGTs was severely restricted due to poor isoform selectivity on–off or blue-shifted fluorescence response. Herein, we established novel “molecular-splicing” strategy construct highly selective near-infrared (NIR) probe, H...

Hydroxylations of pregnenolone (PREG) at the 7 alpha- and 7 beta-positions have been reported in numerous murine tissues and organs and responsible cytochrome P450 (CYP) species await identification. Using thin layer chromatography and gas chromatography-mass spectrometry, we report identification of 7 alpha-hydroxy-PREG and 7 beta-hydroxy-PREG metabolites produced in mouse brain microsome dige...