Protein Information

Name UDP glucuronosyltransferase
Synonyms GNT1; UGT 1; UGT1; GNT1; UDPGT; UDP glucuronosyltransferase; UDP glycosyltransferase 1 family polypeptide A10; UDP glucuronosyltransferase 1 10…

Compound Information

Name 1-naphthol
CAS 1-naphthalenol

Reference List

PubMed Abstract RScore(About this table)
6291111 Zaleski J, Gessner T: Re-investigation of the presence of UDP-glucuronosyltransferase in rat liver mitochondria. Res Commun Chem Pathol Pharmacol. 1982 Aug;37(2):279-92.

In mitochondria the specific activity of UDP-glucuronosyltransferase represented only 7-11% of that found in microsomes, when measured in the presence of various aglycone substrates, including 4-nitrophenol, 4-methylumbelliferone, 1-naphthol, phenolphthalein, testosterone and 17 beta-estradiol.
34(0,1,1,4) Details
6182644 Mackenzie PI, Vaisanen M, Hanninen O: Differential induction of UDP glucuronosyltransferase activities towards various substrates after polycyclic aromatic hydrocarbon administration to rats. Toxicol Lett. 1982 Aug;12(4):259-63.

Administration of the carcinogens, benzo [a] pyrene and 1,2-benzanthracene, increased UDP glucuronosyltransferase activities towards 4-nitrophenol, 3-hydroxybenzo [a] pyrene, 7-hydroxycoumarin and 1-naphthol to a greater extent than did pretreatment with the noncarcinogens, anthracene and phenanthrene.
8(0,0,1,3) Details
6442104 Liu Z, Franklin MR: Separation of four glucuronides in a single sample by high-pressure liquid chromatography and its use in the determination of UDP glucuronosyltransferase activity toward four aglycones. Anal Biochem. 1984 Nov 1;142(2):340-6.

A single-solvent, reverse-phase HPLC system that separates glucuronides has been developed, and its applicability to the separation of glucuronides of four substrates (1-naphthol, morphine, testosterone, and estrone), representative of different UDP-glucuronosyltransferase enzymes, has been demonstrated.
32(0,1,1,2) 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.

On the other hand, studying the kinetics of 1-naphthol glucuronidation yielded more focused results, indicating that residues within segment B (84-147) contribute directly to the K (m) value for this substrate.
7(0,0,0,7) Details
7493919 Yokoi T, Narita M, Nagai E, Hagiwara H, Aburada M, Kamataki T: Inhibition of UDP-glucuronosyltransferase by aglycons of natural glucuronides in kampo medicines using SN-38 as a substrate. Jpn J Cancer Res. 1995 Oct;86(10):985-9.

The inhibitory potencies of these aglycons toward UDP-GT were similar to that of 1-naphthol.
2(0,0,0,2) Details
18004206 Udomuksorn W, Elliot DJ, Lewis BC, Mackenzie PI, Yoovathaworn K, Miners JO: Influence of mutations associated with Gilbert and Crigler-Najjar type II syndromes on the glucuronidation kinetics of bilirubin and other UDP-glucuronosyltransferase 1A substrates. Pharmacogenet Genomics. 2007 Dec;17(12):1017-29.


This work compared the effects of (a) the individual UGT1A1 mutations on the glucuronidation kinetics bilirubin, beta-estradiol, 4-methylumbelliferone (4MU) and 1-naphthol (1NP), and (b) the Y486 mutation, which occurs in the conserved carboxyl terminal domain of UGT1A enzymes, on 4MU, 1NP and naproxen glucuronidation by UGT1A3, UGT1A6 and UGT1A10.
2(0,0,0,2) Details
6805477 Lilienblum W, Walli AK, Bock KW: Differential induction of rat liver microsomal UDP-glucuronosyltransferase activites by various inducing agents. Biochem Pharmacol. 1982 Mar 15;31(6):907-13.

The selectivity of various inducers of UDP-glucuronosyltransferase was investigated in rat liver microsomes and compared with their effect on monooxygenase reactions. (1) Similar to 3-methyl-cholanthrene beta-naphthoflavone selectively stimulated the glucuronidation of 1-naphthol and 4-methylumbelliferone (GT1 substrates). (2) In contrast, DDT preferentially enhanced the glucuronidation of morphine, 4-hydroxybiphenyl (GT2 substrates) and bilirubin, similar to phenobarbital. (3) Colfibric acid and bezafibrate selectively enhanced bilirubin glucuronidation without affecting GT1 and GT2 reactions. (4) Similar to ethoxyquin and Aroclor 1254, trans-stilbene oxide enhanced both GT1 and GT2 activities but not bilirubin glucuronidation. (5) In contrast to 3-methylcholanthrene-type inducers which induce both cytochrome P-450MC and GT1, probably through a common receptor protein, ethoxyquin and trans-stilbene oxide markedly induced GT1 reactions without affecting benzo [a] pyrene monooxygenase.
1(0,0,0,1) Details
15980103 Tochigi Y, Yamashiki N, Ohgiya S, Ganaha S, Yokota H: Isoform-specific expression and induction of udp-glucuronosyltransferase in immunoactivated peritoneal macrophages of the rat. Drug Metab Dispos. 2005 Sep;33(9):1391-8. Epub 2005 Jun 24.

When macrophage cells cultured in plates were exposed to 1-naphthol and 3-hydroxybenzo-[a] pyrene (3-OH-B [a] P), these glucuronides increased in the medium, indicating that macrophages glucuronidated the chemicals.
1(0,0,0,1) Details
6800071 Batt AM, Martin N, Siest G: Induction of group-1 and group-2 UDP-glucuronosyltransferase in microsomes from the livers of C57 Bl/6 mice. Toxicol Lett. 1981 Dec;9(4):355-60.

Phenobarbital and 3-methylcholanthrene were much more potent inducers than the other four compounds. 3-methylcholanthrene stimulated the glucuronidation of 4-nitrophenol, 4-bromophenol, and 4-chlorophenol ("group-1' substrates) more than phenobarbital, whereas phenobarbital stimulated the glucuronidation of 4-hydroxyphenobarbital, menthol, eugenol, 4-hydroxybiphenyl, morphine, 1-borneol, 4-hydroxyphenytoin, and 1,2,3,4-tetrahydro-1-naphthol ("group-2' substrates).
1(0,0,0,1) Details