Substrate Specificity of Opioid Compounds to UDP-Glucuronosyltransferase (UGT), hUGT2B7 and Bovine Microsomal UGT
نویسندگان
چکیده
منابع مشابه
Product inhibition of UDP-glucuronosyltransferase (UGT) enzymes by UDP obfuscates the inhibitory effects of UGT substrates.
Substrates that are specific for certain UDP-glucuronosyltransferase (UGT) isoforms are usually used as specific inhibitors to identify UGT isoforms responsible for the glucuronidation of drugs. 1-Naphthol and 4-nitrophenol are probe substrates for human UGT1A6. In the present study, we found that UGT1A1-catalyzed estradiol 3-O-glucuronide formation and UGT1A4-catalyzed imipramine N-glucuronide...
متن کاملKey amino acid residues responsible for the differences in substrate specificity of human UDP-glucuronosyltransferase (UGT)1A9 and UGT1A8.
Human UDP-glucuronosyltransferase (UGT)1A9 is one of the major isoforms in liver and extrahepatic tissues, catalyzing the glucuronidation of a variety of drugs, dietary constituents, steroids, fatty acids, and bile acids. UGT1A9 shows high amino acid homology with UGT1A7, UGT1A8, and UGT1A10 with overlapping substrate specificity. However, the affinities for substrates are different among them....
متن کاملInhibitory Effect of Sauchinone on UDP-Glucuronosyltransferase (UGT) 2B7 Activity.
Herb-drug interaction (HDI) limits clinical application of herbs and drugs, and inhibition of herbs towards uridine diphosphate (UDP)-glucuronosyltransferases (UGTs) has gained attention as one of the important reasons to cause HDIs. Sauchinone, an active lignan isolated from aerial parts of Saururus chinensis (Saururacease), possesses anti-oxidant, anti-inflammatory, and anti-viral activities....
متن کاملGenotyping of the UDP-glucuronosyltransferase (UGT) 1A7 gene revisited.
Readers are encouraged to write letters to the editor concerning articles that have been published in GASTROENTEROLOGY. Letters that include original, unpublished data will not be considered. Letters should be typewritten and submitted electronically to In 2001 and in 2003, we published 2 studies reporting the role of single nucleotide polymorphisms (SNPs) of the mu-tagen detoxifying UDP glucur...
متن کاملProbe substrate and enzyme source-dependent inhibition of UDP-glucuronosyltransferase (UGT) 1A9 by wogonin.
BACKGROUND Drug-metabolizing enzymes (DMEs) inhibition based drug-drug interaction and herb-drug interaction severely challenge the R&D process of drugs or herbal ingredients. OBJECTIVE To evaluate the inhibition potential of wogonin (an important flavonoid isolated from the root of Scutellaria baicalensis) towards one of the most important phase II DMEs, UDP-glucuronosyltransferase (UGT) 1A9...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Journal of Health Science
سال: 2005
ISSN: 1344-9702,1347-5207
DOI: 10.1248/jhs.51.325