Protein Information

Name UGT1A8
Synonyms GNT1; UGT 1; UGT1; GNT1; UDPGT; UDP glucuronosyltransferase; UDP glucuronosyltransferase 1A8; UDP glycosyltransferase 1 family polypeptide A8…

Compound Information

Name 1-naphthol
CAS 1-naphthalenol

Reference List

PubMed Abstract RScore(About this table)
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
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).
Despite the identical primary structure of the C-terminal halves of the UGT1A isoforms, there were marked differences in the respective K (m) values for UDPGA, ranging from 52 microM for UGT1A6 to 1256 microM for UGT1A8.
1(0,0,0,1) Details
15502008 Webb LJ, Miles KK, Auyeung DJ, Kessler FK, Ritter JK: Analysis of substrate specificities and tissue expression of rat UDP-glucuronosyltransferases UGT1A7 and UGT1A8. Drug Metab Dispos. 2005 Jan;33(1):77-82. Epub 2004 Oct 22.

Other effective UGT1A8 substrates (> 0.1 nmol/mg/min) included 9-OH-benzo [a] pyrene, 1-naphthol, 4-methylumbelliferone, 7-hydroxycoumarin, chrysin, quercetin, 4-nitrophenol, and estriol.
88(1,1,1,8) Details