Protein Information

Name Ugt1a9
Synonyms GNT1; UGT 1; UGT1; GNT1; UDPGT; HLUGP 4; HLUGP4; LUGP 4…

Compound Information

Name 1-naphthol
CAS 1-naphthalenol

Reference List

PubMed Abstract RScore(About this table)
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-glucuronic acid (UDPGA).
82(1,1,1,2) Details
17686537 Leaver MJ, Wright J, Hodgson P, Boukouvala E, George SG: Piscine UDP-glucuronosyltransferase 1B. Aquat Toxicol. 2007 Oct 15;84(3):356-65. Epub 2007 Jul 1.

Expression of a cDNA for plaice UGT1B in cos7 cells resulted in higher 1-naphthol conjugation in cell homogenates compared to steroid conjugation, whilst bilirubin and bile acid conjugation were undetectable.
37(0,1,1,7) Details
20089735 Itaaho K, Laakkonen L, Finel M: How many and which amino acids are responsible for the large activity differences between the highly homologous UDP-glucuronosyltransferases (UGT) 1A9 and UGT1A10?. Drug Metab Dispos. 2010 Apr;38(4):687-96. Epub 2010 Jan 20.

Further mutagenesis and activity assays suggested that Phe117 of UGT1A9 participates in 1-naphthol binding.
35(0,1,1,5) Details
20145913 Donato MT, Montero S, Castell JV, Gomez-Lechon MJ, Lahoz A: Validated assay for studying activity profiles of human liver UGTs after drug exposure: inhibition and induction studies. Anal Bioanal Chem. 2010 Mar;396(6):2251-63. Epub 2010 Feb 10.

The assays are based on analysis and quantification by high-performance liquid chromatography-tandem mass spectrometry of glucuronides formed from selective probe substrates, namely, beta-estradiol (UGT1A1, 3-glucuronide), 1-naphthol (UGT1A6), propofol (UGT1A9), and naloxone (UGT2B7).
31(0,1,1,1) 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 histidine and proline 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.


The conserved N-terminal domain histidine of UGT1A1, UGT1A6, UGT1A9, and UGT2B7 was mutated to proline and leucine 34 of UGT2B10 was substituted with histidine, and the capacity of the wild-type and mutant proteins to glucuronidate 4MU, 1NP, LTG, TFP, and naproxen was characterized.
3(0,0,0,3) Details
18816295 Takahashi H, Maruo Y, Mori A, Iwai M, Sato H, Takeuchi Y: Effect of D256N and Y483D on propofol glucuronidation by human uridine 5'-diphosphate glucuronosyltransferase (UGT1A9). Basic Clin Pharmacol Toxicol. 2008 Aug;103(2):131-6.

For mycophenolic acid, 1-naphthol and naringenin, the D256N variant lowered glucuronidation activity considerably, compared to Y483D.
6(0,0,0,6) Details
15044611 Kurkela M, Morsky S, Hirvonen J, Kostiainen R, Finel M: An active and water-soluble truncation mutant of the human UDP-glucuronosyltransferase 1A9. Mol Pharmacol. 2004 Apr;65(4):826-31.

We have now replaced the 45 C-terminal amino acids of the human UGT1A9, including its trans-membrane helix, with a fusion peptide ending with six His residues.
UGT1A9Sol exhibited a relatively high rate of scopoletin glucuronidation, whereas its activity toward 1-naphthol, entacapone, umbelliferone, and 4-nitrophenol was much lower.
5(0,0,0,5) Details
9990312 Kobayashi T, Yokota H, Ohgiya S, Iwano H, Yuasa A: UDP-glucuronosyltransferase UGT1A7 induced in rat small intestinal mucosa by oral administration of 2-naphthoflavone. Eur J Biochem. 1998 Dec 15;258(3):948-55.

In the rat intestine, UDP-glucuronosyltransferase (UGT) isoforms were highly induced by oral administration of 2-naphthoflavone, as shown by intestinal UGT activity toward 1-naphthol (1-NA).
Using UGT1A6 cDNA as a probe, we obtained three types of clones corresponding to UGT1A2, UGT1A6 and UGT1A7, in a ratio of 1:1:8, from a cDNA library constructed from the 2-naphthoflavone-treated rat intestine.
1(0,0,0,1) Details
12814968 Chen C, Staudinger JL, Klaassen CD: Nuclear receptor, pregname X receptor, is required for induction of UDP-glucuronosyltranferases in mouse liver by pregnenolone-16 alpha-carbonitrile. Drug Metab Dispos. 2003 Jul;31(7):908-15.


In wild-type mice, PCN treatment significantly increased UGT activities toward bilirubin, 1-naphthol, chloramphenicol, thyroxine, and triiodothyronine.
0(0,0,0,0) Details