Details of Drug-Metabolizing Enzyme (DME)

General Information of DME (ID: DME0072)
DME Name UDP-glucuronosyltransferase 1A6 (UGT1A6), Homo sapiens
Synonyms UDP-glucuronosyltransferase family 1 member A6; UDP-glucuronosyltransferase 1-F; UDP-glucuronosyltransferase 1-6; Phenol-metabolizing UDP-glucuronosyltransferase; UDPGT 1-6; UGT-1F; UGT1*6; UGT1-06; UGT1.6; UGT1A6; UGT1F
Gene Name UGT1A6
UniProt ID
UD16_HUMAN
Gene ID
54578
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
Interactome
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       Interactions between Microbiome and DME (MICBIO)                       
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       Interactions between Xenobiotics and DME (XEOTIC)                      
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       Interactions between Host Protein and DME (HOSPPI)                     
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      Click to Show/Hide the Molecular/Functional Data (Sequence/Structure/Pathway/Function) of This DME
Sequence
MACLLRSFQRISAGVFFLALWGMVVGDKLLVVPQDGSHWLSMKDIVEVLSDRGHEIVVVV
PEVNLLLKESKYYTRKIYPVPYDQEELKNRYQSFGNNHFAERSFLTAPQTEYRNNMIVIG
LYFINCQSLLQDRDTLNFFKESKFDALFTDPALPCGVILAEYLGLPSVYLFRGFPCSLEH
TFSRSPDPVSYIPRCYTKFSDHMTFSQRVANFLVNLLEPYLFYCLFSKYEELASAVLKRD
VDIITLYQKVSVWLLRYDFVLEYPRPVMPNMVFIGGINCKKRKDLSQEFEAYINASGEHG
IVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDLL
GHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTSE
DLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHDL
TWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
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 has specificity for phenols.
Full List of Drug(s) Metabolized by This DME
      Drugs Approved by FDA Click to Show/Hide the Full List of Drugs:        15 Drugs
Fospropofol disodium
 Drug Info Approved Monitored anaesthesia care ICD11: N.A. [1]
Mycophenolate mofetil
 Drug Info Approved Crohn disease ICD11: DD70 [2]
Valproic acid
 Drug Info Approved Epilepsy ICD11: 8A60 [3]
Opicapone
 Drug Info Approved Parkinsonism ICD11: 8A00 [4]
Lasofoxifene
 Drug Info Approved Osteoporosis ICD11: FB83 [5]
Naproxen
 Drug Info Approved Rheumatoid arthritis ICD11: FA20 [6]
Phenytoin
 Drug Info Approved Epilepsy ICD11: 8A60 [7]
Aspirin
 Drug Info Approved Myocardial infarction ICD11: BA41 [8]
Propofol
 Drug Info Approved Anaesthesia ICD11: 8E22 [9]
Acetaminophen
 Drug Info Approved Anaesthesia ICD11: 8E22 [10]
Deferiprone
 Drug Info Approved Thalassaemia ICD11: 3A50 [11]
Mycophenolic acid
 Drug Info Approved Crohn disease ICD11: DD70 [2]
Troglitazone
 Drug Info Approved Diabetes mellitus ICD11: 5A10 [12]
Edaravone
 Drug Info Approved Cerebral stroke ICD11: 8B11 [13]
Gaboxadol
 Drug Info Approved Insomnia ICD11: 7A00-7A0Z [14]
      Drugs in Phase 4 Clinical Trial Click to Show/Hide the Full List of Drugs:          1 Drugs
Silymarin
 Drug Info Phase 4 Fatty liver disease ICD11: DB92 [15], [16]
      Drugs in Phase 3 Clinical Trial Click to Show/Hide the Full List of Drugs:          2 Drugs
LAU-7b
 Drug Info Phase 3 Macular degeneration ICD11: 9B78 [17]
BRN-2217626
 Drug Info Phase 3 Female infertility ICD11: GA31 [18]
      Drugs in Phase 2 Clinical Trial Click to Show/Hide the Full List of Drugs:          6 Drugs
ANW-43703
 Drug Info Phase 2/3 Anogenital warts ICD11: 1A95 [19], [20]
Puerarin
 Drug Info Phase 2 Alcohol dependence ICD11: 6C40 [21]
PT2385
 Drug Info Phase 2 Von hippel-lindau disease ICD11: 5A75 [22]
BCP-13498
 Drug Info Phase 2 Anaesthesia ICD11: 8E22 [23]
BIA 3-202
 Drug Info Phase 2 Parkinsonism ICD11: 8A00 [24]
BN-1270
 Drug Info Phase 2 Pulmonary hypertension ICD11: BB01 [25]
      Drugs in Phase 1 Clinical Trial Click to Show/Hide the Full List of Drugs:          1 Drugs
LM-94
 Drug Info Phase 1/2 Cholangitis ICD11: DC13 [26]
      Preclinical/investigative Agents Click to Show/Hide the Full List of Drugs:          8 Drugs
Hydroxyestrone
 Drug Info Investigative Discovery agent ICD: N.A. [18]
UDP-glucuronate
 Drug Info Investigative Discovery agent ICD: N.A. [26]
A-estradiol
 Drug Info Investigative Discovery agent ICD: N.A. [18]
Hydroxyestradiol
 Drug Info Investigative Discovery agent ICD: N.A. [18]
Bilirubin
 Drug Info Investigative Discovery agent ICD: N.A. [18]
BRN-1999480
 Drug Info Investigative Discovery agent ICD: N.A. [18]
Hydroxytryptophol
 Drug Info Investigative Discovery agent ICD: N.A. [27]
Hyodeoxycholic acid
 Drug Info Investigative Discovery agent ICD: N.A. [18]
      Experimental Enzyme Kinetic Data of Drugs Click to Show/Hide the Full List of Drugs:        10 Drugs
BRN-2217626
 Drug Info Phase 3 Female infertility Km = 0.0066 microM [18]
LM-94
 Drug Info Phase 1/2 Cholangitis Km = 0.00012 microM [26]
Hydroxyestrone
 Drug Info Investigative Discovery agent Km = 0.021 microM [18]
UDP-glucuronate
 Drug Info Investigative Discovery agent Km = 0.00025 microM [26]
A-estradiol
 Drug Info Investigative Discovery agent Km = 0.024 microM [18]
Hydroxyestradiol
 Drug Info Investigative Discovery agent Km = 0.01 microM [18]
Bilirubin
 Drug Info Investigative Discovery agent Km = 0.024 microM [18]
BRN-1999480
 Drug Info Investigative Discovery agent Km = 0.014 microM [18]
Hydroxytryptophol
 Drug Info Investigative Discovery agent Km = 0.135 microM [27]
Hyodeoxycholic acid
 Drug Info Investigative Discovery agent Km = 0.011 microM [18]
Full List of Metabolic Reactions (MR) Catalyzed by This DME
MR ID Reactant Product MR Type Source Drug REF
MR000048 Acetaminophen Acetaminophen glucuronide Conjugation - Glucuronidation Acetaminophen [28], [29], [30]
MR006506 ANW-43703 Salicylacyl glucuronide Conjugation - Conjugation ANW-43703 [19], [20]
MR002993 Salicylic acid Phenolic glucuronide Conjugation - Glucuronidation Aspirin [8]
MR002994 Salicylic acid Salicylic acid acyl glucuronide Conjugation - Glucuronidation Aspirin [8]
MR007298 Paracetamol Unclear Unclear - Unclear BCP-13498 [23]
MR007327 BN-1270 Glucuronidation of (+)-cicletanine Conjugation - Glucuronidatioin BN-1270 [25]
MR002940 Deferiprone Deferiprone 3-o glucuronide metabolite Unclear - Unclear Deferiprone [11]
MR000896 Edaravone Edaravone glucuronide conjugates Conjugation - Glucuronidation Edaravone [13]
MR003165 Hydroxyphenytoin Hydroxyphenytoin-O-glucuronide metabolite Unclear - Unclear Fosphenytoin sodium [31]
MR007850 Propofol Propofol-O-glucuronide Conjugation - O-glucuronidation Fospropofol disodium [1]
MR011092 Gaboxadol Gaboxadol-O-glucuronide Conjugation - O-glucuronidation Gaboxadol [14]
MR007053 Hydroxytryptophol 5-Hydroxytryptophol glucuronide Conjugation - Glucuronidation Hydroxytryptophol [27]
MR003709 LAU-7b 4-HPR glucuronide Unclear - Unclear LAU-7b [17]
MR006135 LM-94 4-Methylumbelliferyl glucuronide Conjugation - Conjugation LM-94 [32]
MR004873 O-Desmethylnaproxen O-Desmethylnaproxen acyl glucuronide Conjugation - Glucuronidation Naproxen [33]
MR013702 Opicapone BIA 9-1106 Conjugation - Glucuronidation Opicapone [34]
MR002012 Acetaminophen Acetaminophen glucuronide Conjugation - Glucuronidation Phenacetin [35]
MR002031 Hydroxyphenytoin 4-hydroxyphenytoin o-glucuronide Conjugation - O-Glucuronidation Phenytoin [7], [36]
MR013651 PT2385 PT2385 M8 Conjugation - Glucuronide conjugation PT2385 [22]
MR008594 Puerarin Puerarin-7-O-glucuronide Conjugation - Glucuronidation Puerarin [21]
MR005262 Silymarin 20-O-beta-D-Glu Conjugation - Glucuronidation Silymarin [15], [16]
MR005263 Silymarin Silybin 7-glucoside Conjugation - Glucuronidation Silymarin [15], [16]
MR002497 Valproic acid Valproic acid beta-O-glucuronide metabolite Oxidation - Dehydrogenation Valproic acid [33]
⏷ Show the Full List of 23 MR(s)
References
1 Metabolic Profiles of Propofol and Fospropofol: Clinical and Forensic Interpretative Aspects
2 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
3 UDP glucuronosyltransferase (UGT) 1A6 pharmacogenetics: II. Functional impact of the three most common nonsynonymous UGT1A6 polymorphisms (S7A, T181A, and R184S). J Pharmacol Exp Ther. 2005 Jun;313(3):1340-6.
4 Metabolism and disposition of opicapone in the rat and metabolic enzymes phenotyping
5 DrugBank(Pharmacology-Metabolism):Lasofoxifene
6 S-Naproxen and desmethylnaproxen glucuronidation by human liver microsomes and recombinant human UDP-glucuronosyltransferases (UGT): role of UGT2B7 in the elimination of naproxen. Br J Clin Pharmacol. 2005 Oct;60(4):423-33.
7 Pharmacogenomics knowledge for personalized medicine Clin Pharmacol Ther. 2012 Oct;92(4):414-7. doi: 10.1038/clpt.2012.96.
8 Effect of common single-nucleotide polymorphisms in acetylsalicylic acid metabolic pathway genes on platelet reactivity in patients with diabetes Med Sci Monit. 2013 May 27;19:394-408. doi: 10.12659/MSM.883922.
9 Pharmacokinetics of propofol and extrahepatic UGT1A6 gene expression in anhepatic rats. Pharmacology. 2009;84(4):219-26.
10 UGT1A6 and UGT2B15 polymorphisms and acetaminophen conjugation in response to a randomized, controlled diet of select fruits and vegetables. Drug Metab Dispos. 2011 Sep;39(9):1650-7.
11 Deferiprone glucuronidation by human tissues and recombinant UDP glucuronosyltransferase 1A6: an in vitro investigation of genetic and splice variants. Drug Metab Dispos. 2009 Feb;37(2):322-9.
12 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
13 LABEL:ADICAVA- edaravone injection RADICAVA ORS- edaravone kit
14 Metabolism and renal elimination of gaboxadol in humans: role of UDP-glucuronosyltransferases and transporters
15 Evidence for differences in regioselective and stereoselective glucuronidation of silybin diastereomers from milk thistle (Silybum marianum) by human UDP-glucuronosyltransferases
16 Metabolism, Transport and Drug-Drug Interactions of Silymarin
17 Characterization of the metabolism of fenretinide by human liver microsomes, cytochrome P450 enzymes and UDP-glucuronosyltransferases. Br J Pharmacol. 2011 Feb;162(4):989-99.
18 Structural and functional studies of UDP-glucuronosyltransferases. Drug Metab Rev. 1999 Nov;31(4):817-99.
19 Aromatic hydroxylation of salicylic acid and aspirin by human cytochromes P450. Eur J Pharm Sci. 2015 Jun 20;73:49-56.
20 Polymorphisms of Aspirin-Metabolizing Enzymes CYP2C9, NAT2 and UGT1A6 in Aspirin-Intolerant Urticaria. Allergy Asthma Immunol Res. 2011 Oct;3(4):273-6.
21 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for puerarin metabolism in human liver microsomes
22 Metabolic Profiling of the Novel Hypoxia-Inducible Factor 2 Inhibitor PT2385 In Vivo and In Vitro
23 Human UGT1A6 pharmacogenetics: identification of a novel SNP, characterization of allele frequencies and functional analysis of recombinant allozymes in human liver tissue and in cultured cells. Pharmacogenetics. 2004 Aug;14(8):487-99.
24 Human metabolism of nebicapone (BIA 3-202), a novel catechol-o-methyltransferase inhibitor: characterization of in vitro glucuronidation
25 Induction and inhibition of cicletanine metabolism in cultured hepatocytes and liver microsomes from rats. Fundam Clin Pharmacol. 2000 Sep-Oct;14(5):509-18.
26 Identification of aspartic acid and histidine residues mediating the reaction mechanism and the substrate specificity of the human UDP-glucuronosyltransferases 1A. J Biol Chem. 2007 Dec 14;282(50):36514-24.
27 Evaluation of 5-hydroxytryptophol and other endogenous serotonin (5-hydroxytryptamine) analogs as substrates for UDP-glucuronosyltransferase 1A6. Drug Metab Dispos. 2004 Aug;32(8):862-9.
28 Simultaneous quantification of abemaciclib and its active metabolites in human and mouse plasma by UHPLC-MS/MS J Pharm Biomed Anal. 2021 Sep 5;203:114225. doi: 10.1016/j.jpba.2021.114225.
29 Application of a Volumetric Absorptive Microsampling (VAMS)-Based Method for the Determination of Paracetamol and Four of its Metabolites as a Tool for Pharmacokinetic Studies in Obese and Non-Obese Patients. Clin Pharmacokinet. 2022 Dec;61(12):1719-1733. doi: 10.1007/s40262-022-01187-2.
30 Evaluation of urinary acetaminophen metabolites and its association with the genetic polymorphisms of the metabolising enzymes, and serum acetaminophen concentrations in preterm neonates with patent ductus arteriosus. Xenobiotica. 2021 Nov;51(11):1335-1342. doi: 10.1080/00498254.2021.1982070.
31 U. S. FDA Label -Fosphenytoin sodium
32 Comparisons of detections, stabilities, and kinetics of degradation of hymecromone and its glucuronide and sulfate metabolites
33 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.
34 Pharmacokinetics, pharmacodynamics and tolerability of opicapone, a novel catechol-O-methyltransferase inhibitor, in healthy subjects: prediction of slow enzyme-inhibitor complex dissociation of a short-living and very long-acting inhibitor
35 DrugBank(Pharmacology-Metabolism)Phenacetin
36 Biotransformation of phenytoin in the electrochemically-driven CYP2C19 system. Biophys Chem. 2022 Dec;291:106894. doi: 10.1016/j.bpc.2022.106894.

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