| Name | UGT1A4 |
|---|---|
| Synonyms | Bilirubin specific UDPGT isozyme 2; UGT 1; UGT1; GNT1; UDPGT; HUG BR2; HUGBR 2; HUGBR2… |
| Name | 1-naphthol |
|---|---|
| CAS | 1-naphthalenol |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 17998297 | Fujiwara R, Nakajima M, Yamanaka H, Katoh M, Yokoi T: Product inhibition of UDP-glucuronosyltransferase (UGT) enzymes by UDP obfuscates the inhibitory effects of UGT substrates. Drug Metab Dispos. 2008 Feb;36(2):361-7. Epub 2007 Nov 12. In the present study, we found that UGT1A1-catalyzed 3-O- formation and UGT1A4-catalyzed N- formation in human liver microsomes were prominently decreased in the presence of 1-naphthol, but those by recombinant human UGT1A1 and UGT1A4, respectively, were not. |
88(1,1,2,3) | Details |
| 17636046 | Kubota T, Lewis BC, Elliot DJ, Mackenzie PI, Miners JO: Critical roles of residues 36 and 40 in the and tertiary amine aglycone substrate selectivities of UDP-glucuronosyltransferases 1A3 and 1A4. Mol Pharmacol. 2007 Oct;72(4):1054-62. Epub 2007 Jul 17. UGT1A3 glucuronidates the planar phenols 1-naphthol (1-NP) and 4-methylumbelliferone (4-MU), whereas UGT1A4 converts the tertiary amines (LTG) and trifluoperazine (TFP) to quaternary ammonium glucuronides. |
38(0,1,1,8) | Details |
| 15788539 | Di Marco A, D'Antoni M, Attaccalite S, Carotenuto P, Laufer R: Determination of drug glucuronidation and UDP-glucuronosyltransferase selectivity using a 96-well radiometric assay. Drug Metab Dispos. 2005 Jun;33(6):812-9. Epub 2005 Mar 23. The major UGT isoforms identified were UGT1A6, UGT1A7, and UGT1A9 for 4-methylumbelliferone; UGT1A6 and UGT1A8 for 1-naphthol; UGT2B7 for naloxone; UGT1A3 and UGT2B7 for ketoprofen; and UGT1A4 for trifluoperazine. |
6(0,0,1,1) | Details |
| 19487247 | Kerdpin O, Mackenzie PI, Bowalgaha K, Finel M, Miners JO: Influence of N-terminal domain and residues on the substrate selectivities of human UDP-glucuronosyltransferase 1A1, 1A6, 1A9, 2B7, and 2B10. Drug Metab Dispos. 2009 Sep;37(9):1948-55. Epub 2009 Jun 1. An N-terminal domain [corresponding to position 39 of UDP-glucuronosyltransferase (UGT) 1A1] is conserved in all UGT1A and UGT2B subfamily proteins except UGT1A4 (Pro-40) and UGT2B10 -34). |
5(0,0,0,5) | Details |
| 17301691 | Kurkela M, Patana AS, Mackenzie PI, Court MH, Tate CG, Hirvonen J, Goldman A, Finel M: Interactions with other human UDP-glucuronosyltransferases attenuate the consequences of the Y485D mutation on the activity and substrate affinity of UGT1A6. Pharmacogenet Genomics. 2007 Feb;17(2):115-26. Using 1-naphthol as the aglycone substrate, the Km of 6YD for the cosubstrate UDP- was about 50 times higher than in UGT1A6. RESULTS: Coinfections with UGT1A4 increased the normalized scopoletin glucuronidation of 6YD (the Y485D mutant of UGT1A6) much more than it affected 1YD (the Y486D mutant of UGT1A1). |
2(0,0,0,2) | Details |
| 15802387 | Luukkanen L, Taskinen J, Kurkela M, Kostiainen R, Hirvonen J, Finel M: Kinetic characterization of the 1A subfamily of recombinant human UDP-glucuronosyltransferases. Drug Metab Dispos. 2005 Jul;33(7):1017-26. Epub 2005 Mar 31. The glucuronidation of entacapone by UGT1A9 was inhibited by 1-naphthol in a competitive fashion, with respect to entacapone, and an uncompetitive fashion, with respect to UDP- (UDPGA). The results demonstrated that seven of the UGT1A isoforms are capable of conjugating phenolic substrates with similar highest k (cat) values, and UGT1A4 has a lower relative turnover rate. |
1(0,0,0,1) | Details |
| 15039294 | Uchaipichat V, Mackenzie PI, Guo XH, Gardner-Stephen D, Galetin A, Houston JB, Miners JO: Human udp-glucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid. Drug Metab Dispos. 2004 Apr;32(4):413-23. All isoforms except UGT1A4 glucuronidated 4MU, whereas all but UGT 1A4, 2B15, and 2B17 metabolized 1NP. |
1(0,0,0,1) | Details |