| HOME | HELP | FEEDBACK | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
|
|
|
|||||||
|
|||||||||
(Received for publication, March 11, 1996, and in revised form, May 13, 1996)
From the Medical Research Council Group in Molecular Endocrinology,
CHUL Research Center, Laval University,
Québec G1V 4G2, Canada
To isolate cDNA clones encoding novel UGT2B
enzymes, human prostate and LNCaP cell cDNA libraries were screened
using a pool of steroid-specific UGT2B cDNA probes. In
approximately 106 recombinants, we isolated 3 cDNA
clones of 2.1 kilobases that encode a novel UGT2B enzyme. UGT2B17 is
95% identical with UGT2B15 and 91% identical with UGT2B8. Primary
structure analysis of UGT2B17 based on the nucleotide sequence revealed
a putative amino-terminal membrane insertion signal peptide, a
carboxyl-terminal membrane-spanning region, and three potential
asparagine-linked glycosylation sites. UGT2B17 cloned in the pBK-CMV
expression vector was transfected into HK293 cells to obtain a stable
clonal cell line expressing a high level of the active 53-kDa UGT2B17
enzyme. Of the over 60 endogenous and exogenous substances tested, 25 compounds revealed reactivity. The major substrates are eugenol > 4-methylumbelliferone > dihydrotestosterone > androstane-3
,17
-diol (3-diol) > testosterone > androsterone (ADT). The apparent Km values obtained
with tritiated steroids in intact cells were 0.4 µM for
ADT, 0.7 µM for dihydrotestosterone, 1.0 µM
for 3-diol, and 3.4 µM for testosterone. Southern blot
analysis of reverse transcription-polymerase chain reaction products
revealed expression of UGT2B17 mRNA in various tissues including
the liver, kidney, testis, uterus, placenta, mammary gland, adrenal
gland, skin, and prostate. UGT2B17 is the first human uridine
diphosphoglucuronosyltransferase enzyme expressed in extrahepatic
tissues to have a specificity for ADT as well as testosterone,
dihydrotestosterone, and 3-diol.
CiteULike 
Complore 
Connotea 
Del.icio.us 
Digg 
Reddit 
Technorati What's this?
This article has been cited by other articles:
|
|
 |
|
  C. Swanson, D. Mellstrom, M. Lorentzon, L. Vandenput, J. Jakobsson, A. Rane, M. Karlsson, O. Ljunggren, U. Smith, A.-L. Eriksson, et al. The Uridine Diphosphate Glucuronosyltransferase 2B15 D85Y and 2B17 Deletion Polymorphisms Predict the Glucuronidation Pattern of Androgens and Fat Mass in Men J. Clin. Endocrinol. Metab., December 1, 2007; 92(12): 4878 - 4882. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 S. Chouinard, O. Barbier, and A. Belanger UDP-glucuronosyltransferase 2B15 (UGT2B15) and UGT2B17 Enzymes Are Major Determinants of the Androgen Response in Prostate Cancer LNCaP Cells J. Biol. Chem., November 16, 2007; 282(46): 33466 - 33474. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 C. J. Gallagher, J. E. Muscat, A. N. Hicks, Y. Zheng, A.-M. Dyer, G. A. Chase, J. Richie, and P. Lazarus The UDP-Glucuronosyltransferase 2B17 Gene Deletion Polymorphism: Sex-Specific Association with Urinary 4-(Methylnitrosamino)-1-(3-Pyridyl)-1-Butanol Glucuronidation Phenotype and Risk for Lung Cancer Cancer Epidemiol. Biomarkers Prev., April 1, 2007; 16(4): 823 - 828. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 K. Bowalgaha, D. J. Elliot, P. I. Mackenzie, K. M. Knights, and J. O. Miners The Glucuronidation of {Delta}4-3-Keto C19- and C21-Hydroxysteroids by Human Liver Microsomal and Recombinant UDP-glucuronosyltransferases (UGTs): 6{alpha}- and 21-Hydroxyprogesterone Are Selective Substrates for UGT2B7 Drug Metab. Dispos., March 1, 2007; 35(3): 363 - 370. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
D. B. Buckley and C. D. Klaassen Tissue- and Gender-Specific mRNA Expression of UDP-Glucuronosyltransferases (UGTs) in Mice Drug Metab. Dispos., January 1, 2007; 35(1): 121 - 127. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 S. Chouinard, G. Pelletier, A. Belanger, and O. Barbier Isoform-Specific Regulation of Uridine Diphosphate-Glucuronosyltransferase 2B Enzymes in the Human Prostate: Differential Consequences for Androgen and Bioactive Lipid Inactivation Endocrinology, November 1, 2006; 147(11): 5431 - 5442. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. Park, L. Chen, L. Ratnashinge, T. A. Sellers, J.-P. Tanner, J.-H. Lee, N. Dossett, N. Lang, F. F. Kadlubar, C. B. Ambrosone, et al. Deletion Polymorphism of UDP-Glucuronosyltransferase 2B17 and Risk of Prostate Cancer in African American and Caucasian Men. Cancer Epidemiol. Biomarkers Prev., August 1, 2006; 15(8): 1473 - 1478. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
W. R. Harrington, S. Sengupta, and B. S. Katzenellenbogen Estrogen Regulation of the Glucuronidation Enzyme UGT2B15 in Estrogen Receptor-Positive Breast Cancer Cells Endocrinology, August 1, 2006; 147(8): 3843 - 3850. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
T. Murai, N. Samata, H. Iwabuchi, and T. Ikeda HUMAN UDP-GLUCURONOSYLTRANSFERASE, UGT1A8, GLUCURONIDATES DIHYDROTESTOSTERONE TO A MONOGLUCURONIDE AND FURTHER TO A STRUCTURALLY NOVEL DIGLUCURONIDE Drug Metab. Dispos., July 1, 2006; 34(7): 1102 - 1108. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 R. Obligacion, M. Murray, and I. Ramzan Drug-Metabolizing Enzymes and Transporters: Expression in the Human Prostate and Roles in Prostate Drug Disposition J Androl, March 1, 2006; 27(2): 138 - 150. [Full Text] [PDF]
|
|
|
|
 |
|
 F Labrie, V Luu-The, A Belanger, S-X Lin, J Simard, G Pelletier, and C Labrie Is dehydroepiandrosterone a hormone? J. Endocrinol., November 1, 2005; 187(2): 169 - 196. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
Y. Ishii, A. Miyoshi, D. Maji, H. Yamada, and K. Oguri SIMULTANEOUS EXPRESSION OF GUINEA PIG UDP-GLUCURONOSYLTRANSFERASE 2B21 (UGT2B21) AND 2B22 IN COS-7 CELLS ENHANCES UGT2B21-CATALYZED CHLORAMPHENICOL GLUCURONIDATION Drug Metab. Dispos., October 1, 2004; 32(10): 1057 - 1060. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. Saeki, Y. Saito, H. Jinno, T. Tanaka-Kagawa, A. Ohno, S. Ozawa, K. Ueno, S. Kamakura, N. Kamatani, K. Komamura, et al. SINGLE NUCLEOTIDE POLYMORPHISMS AND HAPLOTYPE FREQUENCIES OF UGT2B4 AND UGT2B7 IN A JAPANESE POPULATION Drug Metab. Dispos., September 1, 2004; 32(9): 1048 - 1054. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
I. Martineau, A. Tchernof, and A. Belanger AMINO ACID RESIDUE ILE211 IS ESSENTIAL FOR THE ENZYMATIC ACTIVITY OF HUMAN UDP-GLUCURONOSYLTRANSFERASE 1A10 (UGT1A10) Drug Metab. Dispos., April 1, 2004; 32(4): 455 - 459. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
D. Wiener, D. R. Doerge, J.-L. Fang, P. Upadhyaya, and P. Lazarus CHARACTERIZATION OF N-GLUCURONIDATION OF THE LUNG CARCINOGEN 4-(METHYLNITROSAMINO)-1-(3-PYRIDYL)-1-BUTANOL (NNAL) IN HUMAN LIVER: IMPORTANCE OF UDP-GLUCURONOSYLTRANSFERASE 1A4 Drug Metab. Dispos., January 1, 2004; 32(1): 72 - 79. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
T. Kuuranne, M. Kurkela, M. Thevis, W. Schanzer, M. Finel, and R. Kostiainen GLUCURONIDATION OF ANABOLIC ANDROGENIC STEROIDS BY RECOMBINANT HUMAN UDP-GLUCURONOSYLTRANSFERASES Drug Metab. Dispos., September 1, 2003; 31(9): 1117 - 1124. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
C. Girard, O. Barbier, G. Veilleux, M. El-Alfy, and A. Belanger Human Uridine Diphosphate-Glucuronosyltransferase UGT2B7 Conjugates Mineralocorticoid and Glucocorticoid Metabolites Endocrinology, June 1, 2003; 144(6): 2659 - 2668. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 D. Turgeon, S. Chouinard, P. Belanger, S. Picard, J.-F. Labbe, P. Borgeat, and A. Belanger Glucuronidation of arachidonic and linoleic acid metabolites by human UDP-glucuronosyltransferases J. Lipid Res., June 1, 2003; 44(6): 1182 - 1191. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. Murata, E. H. Warren, and S. R. Riddell A Human Minor Histocompatibility Antigen Resulting from Differential Expression due to a Gene Deletion J. Exp. Med., May 19, 2003; 197(10): 1279 - 1289. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
D. Turgeon, J.-S. Carrier, S. Chouinard, and A. Belanger Glucuronidation Activity of the UGT2B17 Enzyme toward Xenobiotics Drug Metab. Dispos., May 1, 2003; 31(5): 670 - 676. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 P. A. Gregory and P. I. Mackenzie The Homeodomain Pbx2-Prep1 Complex Modulates Hepatocyte Nuclear Factor 1alpha -Mediated Activation of the UDP-Glucuronosyltransferase 2B17 Gene Mol. Pharmacol., July 1, 2002; 62(1): 154 - 161. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. L. Stanley, R. Hume, T. J. Visser, and M. W. H. Coughtrie Differential Expression of Sulfotransferase Enzymes Involved in Thyroid Hormone Metabolism during Human Placental Development J. Clin. Endocrinol. Metab., December 1, 2001; 86(12): 5944 - 5955. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
R. H. Tukey and C. P. Strassburg Genetic Multiplicity of the Human UDP-Glucuronosyltransferases and Regulation in the Gastrointestinal Tract Mol. Pharmacol., March 1, 2001; 59(3): 405 - 414. [Abstract] [Full Text]
|
|
|
|
|
|
O. Barbier, C. Albert, I. Martineau, M. Vallée, K. High, F. Labrie, D. W. Hum, C. Labrie, and A. Bélanger Glucuronidation of the Nonsteroidal Antiestrogen EM-652 (SCH 57068), by Human and Monkey Steroid Conjugating UDP-Glucuronosyltransferase Enzymes Mol. Pharmacol., March 1, 2001; 59(3): 636 - 645. [Abstract] [Full Text]
|
|
|
|
|
|
D. Turgeon, J.-S. Carrier, E. Levesque, D. W. Hum, and A. Belanger Relative Enzymatic Activity, Protein Stability, and Tissue Distribution of Human Steroid-Metabolizing UGT2B Subfamily Members Endocrinology, February 1, 2001; 142(2): 778 - 787. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
O. Barbier, H. Lapointe, M. El Alfy, D. W. Hum, and A. Bélanger Cellular Localization of Uridine Diphosphoglucuronosyltransferase 2B Enzymes in the Human Prostate by in Situ Hybridization and Immunohistochemistry J. Clin. Endocrinol. Metab., December 1, 2000; 85(12): 4819 - 4826. [Abstract] [Full Text]
|
|
|
|
|
|
P. J. Czernik, J. M. Little, G. W. Barone, J.-P. Raufman, and A. Radominska-Pandya Glucuronidation of Estrogens and Retinoic Acid and Expression of UDP-Glucuronosyltransferase 2B7 in Human Intestinal Mucosa Drug Metab. Dispos., October 1, 2000; 28(10): 1210 - 1216. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
O. Barbier, D. Turgeon, C. Girard, M. D. Green, T. R. Tephly, D. W. Hum, and A. Bélanger 3'-azido-3'-deoxythimidine (AZT) is glucuronidated by human UDP-glucuronosyltransferase 2B7 (UGT2B7) Drug Metab. Dispos., May 1, 2000; 28(5): 497 - 502. [Abstract] [Full Text]
|
|
|
|
|
|
D. O. Hardy, R.-S. Ge, J. F. Catterall, Y.-t. Hou, T. M. Penning, and M. P. Hardy Identification of the Oxidative 3{alpha}-Hydroxysteroid Dehydrogenase Activity of Rat Leydig Cells as Type II Retinol Dehydrogenase Endocrinology, May 1, 2000; 141(5): 1608 - 1617. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
O. Barbier, E. Lévesque, A. Bélanger, and D. W. Hum UGT2B23, a Novel Uridine Diphosphate-Glucuronosyltransferase Enzyme Expressed in Steroid Target Tissues That Conjugates Androgen and Estrogen Metabolites Endocrinology, December 1, 1999; 140(12): 5538 - 5548. [Abstract] [Full Text]
|
|
|
|
|
|
J. Lapointe and C. Labrie Identification and Cloning of a Novel Androgen-Responsive Gene, Uridine Diphosphoglucose Dehydrogenase, in Human Breast Cancer Cells Endocrinology, October 1, 1999; 140(10): 4486 - 4493. [Abstract] [Full Text]
|
|
|
|
|
|
J. Su, X. Chai, B. Kahn, and J. L. Napoli cDNA Cloning, Tissue Distribution, and Substrate Characteristics of a cis-Retinol/3alpha -Hydroxysterol Short-chain Dehydrogenase Isozyme J. Biol. Chem., July 10, 1998; 273(28): 17910 - 17916. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. Levesque, M. Beaulieu, C. Guillemette, D. W. Hum, and A. Belanger Effect of Interleukins on UGT2B15 and UGT2B17 Steroid Uridine Diphosphate-Glucuronosyltransferase Expression and Activity in the LNCaP Cell Line Endocrinology, May 1, 1998; 139(5): 2375 - 2381. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. D. Green, G. Bélanger, D. W. Hum, A. Bélanger, and T. R. Tephly Glucuronidation of Opioids, Carboxylic Acid-Containing Drugs, and Hydroxylated Xenobiotics Catalyzed by Expressed Monkey UDP-Glucuronosyltransferase 2B9 Protein Drug Metab. Dispos., December 1, 1997; 25(12): 1389 - 1394. [Abstract] [Full Text]
|
|
|
|
|
|
C. Guillemette, E. Levesque, M. Beaulieu, D. Turgeon, D. W. Hum, and A. Belanger Differential Regulation of Two Uridine Diphospho-Glucuronosyltransferases, UGT2B15 and UGT2B17, in Human Prostate LNCaP Cells Endocrinology, July 1, 1997; 138(7): 2998 - 3005. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. G. Biswas and D. W. Russell Expression Cloning and Characterization of Oxidative 17beta - and 3alpha -Hydroxysteroid Dehydrogenases from Rat and Human Prostate J. Biol. Chem., June 20, 1997; 272(25): 15959 - 15966. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Tchernof, F. Labrie, A. Belanger, D. Prud'homme, C. Bouchard, A. Tremblay, A. Nadeau, and J.-P. Despres Androstane-3{alpha},17{beta}-Diol Glucuronide as a Steroid Correlate of Visceral Obesity in Men J. Clin. Endocrinol. Metab., May 1, 1997; 82(5): 1528 - 1534. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
C. P. Strassburg, S. Kneip, J. Topp, P. Obermayer-Straub, A. Barut, R. H. Tukey, and M. P. Manns Polymorphic Gene Regulation and Interindividual Variation of UDP-glucuronosyltransferase Activity in Human Small Intestine J. Biol. Chem., November 10, 2000; 275(46): 36164 - 36171. [Abstract] [Full Text] [PDF]
|
|
| HOME | HELP | FEEDBACK | SUBSCRIPTIONS | ARCHIVE | SEARCH | TABLE OF CONTENTS |
| All ASBMB Journals | Molecular and Cellular Proteomics |
| Journal of Lipid Research | ASBMB Today |
