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Activity of rat UGT1A1 towards benzo[a]pyrene phenols and dihydrodiols.
MedLine Citation:
PMID:  21783661     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
Four UDP-glucuronosyltransferases from the rat UGT1A family were tested for activity towards benzo[a]pyrene phenols and dihydrodiols. UGT1A1 and UGT1A7 were found to be broadly active towards BaP metabolites. Antisera recognizing rat UGT1A1 and UGT1A7 were used to assess UGT levels in relation to UGT activity towards benzo[a]pyrene-7,8-dihydrodiol (BPD). The rank BPD UGT activities were liver=intestine≫kidney, whereas UGT1A1 was highest in liver and UGT1A7 was highest in intestine. Phenobarbital, an inducer of hepatic UGT1A1, only slightly increased BPD UGT activity, whereas UGT1A7 inducers more potently increased the activity. Inhibition studies using the differential UGT1A1 inhibitor, bilirubin, suggest that UGT1A1 is not a major contributor to the constitutive BPD glucuronidating activity of control rat liver microsomes. These data suggest that multiple UGT1A enzymes contribute to glucuronidation of BPD and other BaP metabolites, and that their relative contributions depend on tissue- and environmental-specific factors.
Authors:
Laura Webb; Kristini Miles; Fay Kessler; Joseph K Ritter
Publication Detail:
Type:  Journal Article     Date:  2005-11-02
Journal Detail:
Title:  Environmental toxicology and pharmacology     Volume:  21     ISSN:  1382-6689     ISO Abbreviation:  Environ. Toxicol. Pharmacol.     Publication Date:  2006 May 
Date Detail:
Created Date:  2011-07-25     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9612020     Medline TA:  Environ Toxicol Pharmacol     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  224-30     Citation Subset:  -    
Affiliation:
Department of Pharmacology and Toxicology, Virginia Commonwealth University School of Medicine, Campus Box 980613, 1217 E. Marshall Room 536, Richmond, VA 23298-0613, USA.
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