Regulation of the human UGT1A1 gene by nuclear receptors constitutive active/androstane receptor, pregnane X receptor, and glucocorticoid receptor.
作者： Junko Sugatani , Tatsuya Sueyoshi , Masahiko Negishi , Masao Miwa
DOI: 10.1016/S0076-6879(05)00006-6
关键词: Pregnane X receptor 、 Nuclear receptor coactivator 2 、 Chemistry 、 5-HT5A receptor 、 Nuclear receptor 、 Estrogen-related receptor alpha 、 Liver X receptor beta 、 Constitutive androstane receptor 、 Pharmacology 、 Biochemistry 、 Estrogen-related receptor gamma
摘要: Abstract Human UDP‐glucuronosyltransferase (UGT) 1A1 is the enzyme that detoxifies neurotoxic bilirubin by conjugating it with glucuronic acid. In addition to bilirubin, UGT1A1 conjugates various endogenous and exogenous lipophilic compounds such as estrogens active metabolite of anticancer drug irinotecan SN‐38. Thus, activation specific inducers gene critical in treating patients unconjugated hyperbili‐rubinemia preventing side effects treatment SN‐38‐induced toxicity. This chapter describes experimental processes used identify 290‐bp distal enhancer module at −3499/−3210 characterize its regulation nuclear receptors: constitutive active/androstane receptor, pregnane X glucocorticoid receptor.
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