RRC ID |
42530
|
Author |
Sugatani J, Sueyoshi T, Negishi M, Miwa M.
|
Title |
Regulation of the human UGT1A1 gene by nuclear receptors constitutive active/androstane receptor, pregnane X receptor, and glucocorticoid receptor.
|
Journal |
Methods Enzymol
|
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 and the active metabolite of the anticancer drug irinotecan SN-38. Thus, activation by specific inducers of the UGT1A1 gene is critical in treating patients with unconjugated hyperbili-rubinemia and in preventing side effects of drug treatment such as SN-38-induced toxicity. This chapter describes the experimental processes used to identify the 290-bp distal enhancer module at -3499/-3210 of the UGT1A1 gene and to characterize its regulation by nuclear receptors: constitutive active/androstane receptor, pregnane X receptor, and glucocorticoid receptor.
|
Volume |
400
|
Pages |
92-104
|
Published |
2005-1-1
|
DOI |
10.1016/S0076-6879(05)00006-6
|
PII |
S0076-6879(05)00006-6
|
PMID |
16399345
|
MeSH |
Binding Sites
Constitutive Androstane Receptor
Electrophoretic Mobility Shift Assay
Enhancer Elements, Genetic*
Gene Expression Regulation, Enzymologic*
Glucuronosyltransferase / genetics*
Glucuronosyltransferase / metabolism
Humans
Mutagenesis, Site-Directed
Pregnane X Receptor
RNA, Messenger / biosynthesis
Receptors, Cytoplasmic and Nuclear / genetics*
Receptors, Cytoplasmic and Nuclear / metabolism
Receptors, Glucocorticoid / genetics*
Receptors, Glucocorticoid / metabolism
Receptors, Steroid / genetics*
Receptors, Steroid / metabolism
Transcription Factors / genetics*
Transcription Factors / metabolism
|
IF |
1.394
|
Times Cited |
41
|
WOS Category
|
BIOCHEMICAL RESEARCH METHODS
BIOCHEMISTRY & MOLECULAR BIOLOGY
|
Resource |
Human and Animal Cells |
Hep G2(RCB1648) |