Protein Information

Name udp glucuronosyltransferase 2B7
Synonyms UDP glucuronosyltransferase 2B7; UDPGT; UDP glucuronosyltransferase 2B7 precursor; UDPGTh 2; UGT2B7; UGT2B7 protein; UGT2B9; UGTB2B9…

Compound Information

Name 1-naphthol
CAS 1-naphthalenol

Reference List

PubMed Abstract RScore(About this table)
18647858 Uchaipichat V, Galetin A, Houston JB, Mackenzie PI, Williams JA, Miners JO: Kinetic modeling of the interactions between 4-methylumbelliferone, 1-naphthol, and zidovudine glucuronidation by udp-glucuronosyltransferase 2B7 (UGT2B7) provides evidence for multiple substrate binding and effector sites. Mol Pharmacol. 2008 Oct;74(4):1152-62. Epub 2008 Jul 22.
85(1,1,1,5) 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).
32(0,1,1,2) Details
9364930 Belanger G, Beaulieu M, Levesque E, Hum DW, Belanger A: Expression and characterization of a novel UDP-glucuronosyltransferase, UGT2B9, from cynomolgus monkey. DNA Cell Biol. 1997 Oct;16(10):1195-205.

The activity of UGT2B9 was tested with over 60 compounds and was demonstrated to be active on C18, C19, and C21 steroids, bile acids, and several xenobiotics including eugenol, 1-naphthol, and p-nitrophenol.
10(0,0,1,5) 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.
2(0,0,0,2) Details
10901286 Sabolovic N, Magdalou J, Netter P, Abid A: Nonsteroidal anti-inflammatory drugs and phenols glucuronidation in Caco-2 cells: identification of the UDP-glucuronosyltransferases UGT1A6, 1A3 and 2B7. Life Sci. 2000;67(2):185-96.

Glucuronidation of phenols (1-naphthol, 4-methylumbelliferone) and nonsteroidal anti-inflammatory drugs (NSAIDs) such as ketoprofen, naproxen and carprofen was investigated in human colon carcinoma Caco-2 cell clones.
RT-PCR experiments indicated that the PD-7 and TC-7 clones expressed the UDP-glucuronosyltransferase (UGT) isoforms UGT1A6, UGT1A3 and UGT2B7, which could account for the glucuronidation of phenols and carboxylic acids observed.
2(0,0,0,2) 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-glucuronic acid was about 50 times higher than in UGT1A6.
Coexpression also influenced wild-type UGT1A6 and UGT2B7, increasing the normalized activity of UGT1A6, but decreasing it for UGT2B7.
1(0,0,0,1) Details