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Literature summary for 2.4.1.17 extracted from

  • Bushey, R.T.; Chen, G.; Blevins-Primeau, A.S.; Krzeminski, J.; Amin, S.; Lazarus, P.
    Characterization of UDP-glucuronosyltransferase 2A1 (UGT2A1) variants and their potential role in tobacco carcinogenesis (2011), Pharmacogenet. Genomics, 21, 55-65.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine isoform UGT2A1 is an important detoxification enzyme in the metabolism of polycyclic aromatic hydrocarbons within target tissues for tobacco carcinogens, and functional polymorphisms in UGT2A1 may play a role in tobacco-related cancer risk Homo sapiens

Protein Variants

Protein Variants Comment Organism
K75R single nucleotide polymorphism, about 25% decrease in glucuronidation activity Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.03
-
1-naphthol wild-type, pH 7.4, 37°C Homo sapiens
0.044
-
1-naphthol mutant K75R, pH 7.4, 37°C Homo sapiens
0.091
-
1-hydroxypyrene wild-type, pH 7.4, 37°C Homo sapiens
0.111
-
1-hydroxypyrene mutant K75R, pH 7.4, 37°C Homo sapiens
0.247
-
1-hydroxy-benzo(a)pyrene wild-type, pH 7.4, 37°C Homo sapiens
0.261
-
7-hydroxy-benzo(a)pyrene wild-type, pH 7.4, 37°C Homo sapiens
0.263
-
1-hydroxy-benzo(a)pyrene mutant K75R, pH 7.4, 37°C Homo sapiens
0.27
-
5-methylchrysene-1,2-diol wild-type, pH 7.4, 37°C Homo sapiens
0.271
-
3-hydroxy-benzo(a)pyrene wild-type, pH 7.4, 37°C Homo sapiens
0.278
-
3-hydroxy-benzo(a)pyrene mutant K75R, pH 7.4, 37°C Homo sapiens
0.284
-
dibenzo(a,l)pyrene-11,12-diol wild-type, pH 7.4, 37°C Homo sapiens
0.307
-
dibenzo(a,l)pyrene-11,12-diol mutant K75R, pH 7.4, 37°C Homo sapiens
0.308
-
8-hydroxy-benzo(a)pyrene wild-type, pH 7.4, 37°C Homo sapiens
0.334
-
7-hydroxy-benzo(a)pyrene mutant K75R, pH 7.4, 37°C Homo sapiens
0.368
-
8-hydroxy-benzo(a)pyrene mutant K75R, pH 7.4, 37°C Homo sapiens
0.381
-
5-methylchrysene-1,2-diol mutant K75R, pH 7.4, 37°C Homo sapiens
0.397
-
benzo(a)pyrene-7,8-diol wild-type, pH 7.4, 37°C Homo sapiens
0.426
-
benzo(a)pyrene-7,8-diol mutant K75R, pH 7.4, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
colon isoform UGT2A1 is expressed in aerodigestive tract tissues including trachea, larynx and tonsil, and is also expressed in lung and colon. Isoform UGT2A1 exhibits highest expression in the lung, followed in decreasing order by trachea, tonsil, larynx, colon, olfactory tissue Homo sapiens
-
larynx isoform UGT2A1 is expressed in aerodigestive tract tissues including trachea, larynx and tonsil, and is also expressed in lung and colon. Isoform UGT2A1 exhibits highest expression in the lung, followed in decreasing order by trachea, tonsil, larynx, colon, olfactory tissue Homo sapiens
-
lung isoform UGT2A1 is expressed in aerodigestive tract tissues including trachea, larynx and tonsil, and is also expressed in lung and colon. Isoform UGT2A1 exhibits highest expression in the lung, followed in decreasing order by trachea, tonsil, larynx, colon, olfactory tissue Homo sapiens
-
additional information no expression of isoform UGT2A1 in breast, whole brain, pancreas, prostate, kidney, liver or esophagus Homo sapiens
-
tonsil isoform UGT2A1 is expressed in aerodigestive tract tissues including trachea, larynx and tonsil, and is also expressed in lung and colon. Isoform UGT2A1 exhibits highest expression in the lung, followed in decreasing order by trachea, tonsil, larynx, colon, olfactory tissue Homo sapiens
-
trachea isoform UGT2A1 is expressed in aerodigestive tract tissues including trachea, larynx and tonsil, and is also expressed in lung and colon. Isoform UGT2A1 exhibits highest expression in the lung, followed in decreasing order by trachea, tonsil, larynx, colon, olfactory tissue Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-hydroxy-benzo(a)pyrene + UDP-glucuronate
-
Homo sapiens 1-hydroxy-benzo(a)pyrene 1-O-glucuronate + UDP
-
?
1-hydroxypyrene + UDP-glucuronate
-
Homo sapiens 1-hydroxypyrene 1-O-glucuronate + UDP
-
?
1-naphthol + UDP-glucuronate
-
Homo sapiens 1-naphthyl 1-O-glucuronate + UDP
-
?
3-hydroxy-benzo(a)pyrene + UDP-glucuronate
-
Homo sapiens 3-hydroxy-benzo(a)pyrene 3-O-glucuronate + UDP
-
?
5-methylchrysene-1,2-diol + UDP-glucuronate
-
Homo sapiens ? + UDP
-
?
7-hydroxy-benzo(a)pyrene + UDP-glucuronate
-
Homo sapiens 7-hydroxy-benzo(a)pyrene 7-O-glucuronate + UDP
-
?
8-hydroxy-benzo(a)pyrene + UDP-glucuronate
-
Homo sapiens 8-hydroxy-benzo(a)pyrene 8-O-glucuronate + UDP
-
?
benzo(a)pyrene-7,8-diol + UDP-glucuronate
-
Homo sapiens ? + UDP
-
?
dibenzo(a,l)pyrene-11,12-diol + UDP-glucuronate
-
Homo sapiens ? + UDP
-
?
additional information isoform UGT2A1 is not active with substrates that form N-glucuronides, such as 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol, nicotine, or N-hydroxy-2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine Homo sapiens ?
-
?