Details of Drug-Metabolizing Enzyme (DME)

General Information of DME (ID: DME0622)
DME Name UDP-glucuronosyltransferase 2A1 (UGT2A1), Homo sapiens
Synonyms UDP-glucuronosyltransferase family 2 member A1; UDPGT 2A1; UGT2A1; UGT2A2; OMIM: 604716; MGI: 2149905; HomoloGene: 136808; GeneCards: UGT2A1
Gene Name UGT2A1
UniProt ID
UD2A1_HUMAN
Gene ID
574537
EC Number    EC: 2.4.1.17     (Click to Show/Hide the Complete EC Tree)
Transferase
Glycosyltransferases
Hexosyltransferase
EC: 2.4.1.17
Lineage    Species: Homo sapiens     (Click to Show/Hide the Complete Species Lineage)
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
      Click to Show/Hide the Molecular/Functional Data (Sequence/Structure/Pathway/Function) of This DME
Sequence
MLNNLLLFSLQISLIGTTLGGNVLIWPMEGSHWLNVKIIIDELIKKEHNVTVLVASGALF
ITPTSNPSLTFEIYRVPFGKERIEGVIKDFVLTWLENRPSPSTIWRFYQEMAKVIKDFHM
VSQEICDGVLKNQQLMAKLKKSKFEVLVSDPVFPCGDIVALKLGIPFMYSLRFSPASTVE
KHCGKVPYPPSYVPAVLSELTDQMSFTDRIRNFISYHLQDYMFETLWKSWDSYYSKALGR
PTTLCETMGKAEIWLIRTYWDFEFPRPYLPNFEFVGGLHCKPAKPLPKEMEEFIQSSGKN
GVVVFSLGSMVKNLTEEKANLIASALAQIPQKVLWRYKGKKPATLGNNTQLFDWIPQNDL
LGHPKTKAFITHGGTNGIYEAIYHGVPMVGVPMFADQPDNIAHMKAKGAAVEVNLNTMTS
VDLLSALRTVINEPSYKENAMRLSRIHHDQPVKPLDRAVFWIEFVMRHKGAKHLRVAAHD
LTWFQYHSLDVIGFLLVCVTTAIFLVIQCCLFSCQKFGKIGKKKKRE
Pathway Ascorbate and aldarate metabolism (hsa00053 )
Chemical carcinogenesis (hsa05204 )
Drug metabolism - cytochrome P450 (hsa00982 )
Drug metabolism - other enzymes (hsa00983 )
Metabolic pathways (hsa01100 )
Metabolism of xenobiotics by cytochrome P450 (hsa00980 )
Pentose and glucuronate interconversions (hsa00040 )
Porphyrin and chlorophyll metabolism (hsa00860 )
Retinol metabolism (hsa00830 )
Steroid hormone biosynthesis (hsa00140 )
Function This enzyme catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase water solubility and enhance excretion. And it is important in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.
Full List of Drug(s) Metabolized by This DME
      Drugs Approved by FDA Click to Show/Hide the Full List of Drugs:          6 Drugs
Methyltestosterone
 Drug Info Approved Breast cancer ICD11: 2C60 [1]
Nateglinide
 Drug Info Approved Diabetes mellitus ICD11: 5A10 [2]
Nevirapine
 Drug Info Approved Human immunodeficiency virus infection ICD11: 1C60 [3]
Dronedarone hydrochloride
 Drug Info Approved Atrial fibrillation ICD11: BC81 [4]
Fluoxetine hydrochloride
 Drug Info Approved Depression ICD11: 6A71 [5]
Oxymetazoline
 Drug Info Approved Erythema multiforme ICD11: EB12 [6]
Full List of Metabolic Reactions (MR) Catalyzed by This DME
MR ID Reactant Product MR Type Source Drug REF
MR009678 Curcumin Curcumin bate-O-glucuronide Conjugation - Glucuronidation Curcumin [2], [7]
MR009670 Dihydrocurcumin Dihydrocurcumin bate-O-glucuronide Conjugation - Glucuronidation Curcumin [2]
MR009676 Hexahydrocurcumin Hexahydrocurcumin bate-O-glucuronide Conjugation - Glucuronidation Curcumin [2]
MR009674 Tetrahydrocurcumin Tetrahydrocurcumin bate-O-glucuronide Conjugation - Glucuronidation Curcumin [2]
MR006703 Deaminated N,N-didebutyl-dronedarone Deaminated N,N-didebutyl-dronedarone glucuronide Conjugation - Glucuronidation Dronedarone hydrochloride [4]
MR005019 Fluoxetine hydrochloride Fluoxetine glucuronide Conjugation - Glucuronidation Fluoxetine hydrochloride [2]
MR005017 Norfluoxetine Norfluoxetine glucuronide Conjugation - Glucuronidation Fluoxetine hydrochloride [5]
MR004882 Nateglinide Nateglinide glucuronide and isomers (M4/M5/M6) Conjugation - Glucuronidation Nateglinide [2]
MR003158 Oxymetazoline Oxymetazoline O-glucuronidation Conjugation - O-Glucuronidation Oxymetazoline [8], [6]
⏷ Show the Full List of 9 MR(s)
References
1 Hepatic expression patterns of aryl hydrocarbon receptor, pregnane X receptor, two cytochrome P450s and five phase II metabolism genes responsive to 17alpha-methyltestosterone in rare minnow Gobiocypris rarus. Environ Toxicol Pharmacol. 2014 May;37(3):1157-68.
2 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
3 Sulfation of 12-hydroxy-nevirapine by human SULTs and the effects of genetic polymorphisms of SULT1A1 and SULT2A1. Biochem Pharmacol. 2022 Oct;204:115243. doi: 10.1016/j.bcp.2022.115243.
4 DrugBank(Pharmacology-Metabolism):Dronedarone hydrochloride
5 Pharmacogenomics knowledge for personalized medicine Clin Pharmacol Ther. 2012 Oct;92(4):414-7. doi: 10.1038/clpt.2012.96.
6 Identification and characterization of oxymetazoline glucuronidation in human liver microsomes: evidence for the involvement of UGT1A9. J Pharm Sci. 2011 Feb;100(2):784-93.
7 Curcumin and Weight Loss: Does It Work?
8 In vitro metabolism of oxymetazoline: evidence for bioactivation to a reactive metabolite. Drug Metab Dispos. 2011 Apr;39(4):693-702.

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