Glucuronosyltransferase (UGT) is a glycosyltransferase (EC 220.127.116.11) also known as UDP-glucuronosyltransferase, that catalyzes the addition of a glycosyl group from a UTP-sugar to a small hydrophobic molecule.
Although the majority of UGT enzymes are expressed in the liver, UGT1A7, UGT1A8, and UGT1A10 are expressed exclusively extrahepatically, mainly in the intestine. UGT1A9, UGT2B7, and UGT2B11 are expressed at relatively high amounts in the kidney.
Glucuronosyltransferase catalyzes the conversion of 1-naphthol + UDPglucuronate to 1-naphthyl-O-glucuronide + UDP.
1. In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation.
Zhang D, Chando TJ, Everett DW, Patten CJ, Dehal SS, Humphreys WG. PubMed: PMID: 16118329
2. Effect of valerian, valerian/hops extracts, and valerenic acid on glucuronidation in vitro.
Alkharfy KM, Frye RF. PubMed: PMID: 17484515
3. Inhibitory effects of commonly used herbal extracts on UDP-glucuronosyltransferase 1A4, 1A6, and 1A9 enzyme activities.
Mohamed ME, Frye RF. PubMed: PMID: 21632963
4. Methadone inhibits CYP2D6 and UGT2B7/2B4 in vivo: a study using codeine in methadone- and buprenorphine-maintained subjects.
Gelston EA, Coller JK, Lopatko OV, James HM, Schmidt H, White JM, Somogyi AA. PubMed: PMID: 22092298
5. In vitro-in vivo extrapolation predicts drug-drug interactions arising from inhibition of codeine glucuronidation by dextropropoxyphene, fluconazole, ketoconazole, and methadone in humans.
Raungrut P, Uchaipichat V, Elliot DJ, Janchawee B, Somogyi AA, Miners JO. PubMed: PMID: 20484152
6. Effects of herbal supplements on drug glucuronidation. Review of clinical, animal, and in vitro studies.
Mohamed ME, Frye RF. PubMed: PMID: 21049395
7. Strong inhibition of celastrol towards UDP-glucuronosyl transferase (UGT) 1A6 and 2B7 indicating potential risk of UGT-based herb-drug interaction.
Zhang YS, Tu YY, Gao XC, Yuan J, Li G, Wang L, Deng JP, Wang Q, Ma RM. PubMed: PMID: 22669039
8. Isoliquiritigenin showed strong inhibitory effects towards multiple UDP-glucuronosyltransferase (UGT) isoform-catalyzed 4-methylumbelliferone (4-MU) glucuronidation.
Lu H, Fang ZZ, Cao YF, Hu CM, Hong M, Sun XY, Li H, Liu Y, Fu X, Sun H. PubMed: PMID: 23237733
9. Deglycosylation of Liquiritin Strongly Enhances its Inhibitory Potential Towards UDP-Glucuronosyltransferase (UGT) Isoforms.
Guo B, Fan XR, Fang ZZ, Cao YF, Hu CM, Yang J, Zhang YY, He RR, Zhu X, Yu ZW, Sun XY, Hong M, Yang L. PubMed: PMID: 23065713
10. Glycyrrhetinic Acid Exhibits Strong Inhibitory Effects Towards UDP-Glucuronosyltransferase (UGT) 1A3 and 2B7.
Huang YP, Cao YF, Fang ZZ, Zhang YY, Hu CM, Sun XY, Yu ZW, Zhu X, Hong M, Yang L, Sun HZ. PubMed: PMID: 23148031
11. Effects of Andrographis paniculata and Orthosiphon stamineus extracts on the glucuronidation of 4-methylumbelliferone in human UGT isoforms.
Ismail S, Hanapi NA, Ab Halim MR, Uchaipichat V, Mackenzie PI. PubMed: PMID: 20657500
12. Identification of human UDP-glucuronosyltransferase isoform(s) responsible for the glucuronidation of 2-(4-chlorophenyl)- 5-(2-furyl)-4-oxazoleacetic acid (TA-1801A).
Kaji H, Kume T. PubMed: PMID: 15988124
13. Inhibition of morphine glucuronidation in the liver microsomes of rats and humans by monoterpenoid alcohols.
Ishii Y, Iida N, Miyauchi Y, Mackenzie PI, Yamada H. PubMed: PMID: 22878261
14. Steviol glucuronidation and its potential interaction with UDP-glucuronosyltransferase 2B7 substrates.
Wang M, Lu J, Li J, Qi H, Wang Y, Zhang H.; Food Chem Toxicol. 2014 Feb;64:135-43. doi: 10.1016/j.fct.2013.11.028. Epub 2013 Dec 1.; PMID: 24296138; DOI: 10.1016/j.fct.2013.11.028