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Expression of human liver 3, 4-catechol estrogens UDP-glucuronosyltransferase cDNA in COS 1 cells

Title
Expression of human liver 3, 4-catechol estrogens UDP-glucuronosyltransferase cDNA in COS 1 cells
Authors
Ahn M.R.Owens I.S.Sheen Y.Y.
Ewha Authors
신윤용
SCOPUS Author ID
신윤용scopus
Issue Date
1997
Journal Title
Archives of Pharmacal Research
ISSN
0253-6269JCR Link
Citation
Archives of Pharmacal Research vol. 20, no. 5, pp. 465 - 470
Indexed
SCIE; SCOPUS; KCI scopus
Document Type
Article
Abstract
The human cDNA clone UDPGTh2, encoding a liver UDP-glucuronosyltransferase (UDPGT), was isolated from a λgt 11 cDNA library by hybridization to mouse transferase cDNA clone, UDPGTm1. The two clones had 74% nucleotide sequence identities in the coding region. UDPGTh2 encoded a 529 amino acid protein with an amino terminus membrane-insertion signal peptide and a carboxyl terminus membrane-spanning region. In order to establish substrate specificity, the clone was inserted into the pSVL vector (pUDPGTh2) and expressed in COS 1 cells. Sixty potential substrates were tested using cells transfected with pUDPGTh2. The order of relative substrate activity was as follows: 4-hydroxyestrone > estriol >2-hydroxyestriol > 4-hydroxyestradiol > 6α-hydroxyestradiol > 5α-androstane-3α, 11β, 17β-triol= 5β-androstane-3α, 11β, 17β-triol. There were only trace amounts of gulcuronidation of 2-hydroxyestradiol and 2-hydroxyestrone, and in contrast to other cloned transferase, no gulcuronidation of either the primary estrogens and androgens (estrone, 17β-estradiol/testosterone, androsterone) or any of the exogenous substrates tested was detected. A lineweaver-Burk plot of the effect of 4-hydroxyestrone concentration on the velocity of glucuronidation showed an apparent Km of 13 μM. The unique specificity of this transferase might play an important role in regulating the level and activity of these potent and active estrogen metabolites.
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약학대학 > 약학과 > Journal papers
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