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Literature summary for 2.4.1.17 extracted from
- S-Naproxen and desmethylnaproxen glucuronidation by human liver microsomes and recombinant human UDP-glucuronosyltransferases (UGT): role of UGT2B7 in the elimination of naproxen (2005), Br. J. Clin. Pharmacol., 60, 423-433.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression in HEK-293 cells | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| fluconazole | 2.5 mM, 0.075 mM naproxen, 72% inhibition | Homo sapiens |  |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.072 | - |
naproxen | 37°C, pH 7.4 | Homo sapiens | |
| 0.855 | - |
naproxen | 37°C, pH 7.4 | Homo sapiens | |
| 3.133 | - |
desmethylnaproxen | 37°C, pH 7.4 | Homo sapiens | |
| 3.384 | - |
desmethylnaproxen | 37°C, pH 7.4 | Homo sapiens | |
| 4.375 | - |
naproxen | 37°C, pH 7.4 | Homo sapiens | |
| 7.724 | - |
desmethylnaproxen | 37°C, pH 7.4 | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Homo sapiens | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| UDPglucuronate + naproxen | Homo sapiens | UGT2B7 is responsible for human hepatic naproxen acyl glucuronidation, which is the primary elimination pathway for this drug | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | O60656 | - |
- |
| Homo sapiens | P16662 | - |
- |
| Homo sapiens | P19224 | - |
- |
| Homo sapiens | P22309 | - |
- |
| Homo sapiens | P35503 | - |
- |
| Homo sapiens | Q9HAW7 | - |
- |
| Homo sapiens | Q9HAW9 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| UDP-glucuronate + desmethylnaproxen | UGT 1A3 forms only the acyl glucuronide | Homo sapiens | ? | - |
? | |
| UDP-glucuronate + desmethylnaproxen | UGT 1A6 forms only the acyl glucuronide | Homo sapiens | ? | - |
? | |
| UDP-glucuronate + desmethylnaproxen | UGT1A1 catalyzes both the phenolic and acyl glucuronidation of desmethylnaproxen | Homo sapiens | ? | - |
? | |
| UDP-glucuronate + desmethylnaproxen | UGT1A7 catalyzes both the phenolic and acyl glucuronidation of desmethylnaproxen UGT 1A6 forms only the acyl glucuronide | Homo sapiens | ? | - |
? | |
| UDP-glucuronate + desmethylnaproxen | UGT1A9 catalyzes both the phenolic and acyl glucuronidation of desmethylnaproxen UGT 1A6 forms only the acyl glucuronide | Homo sapiens | ? | - |
? | |
| UDP-glucuronate + desmethylnaproxen | UGT2B7 forms only the acyl glucuronide | Homo sapiens | ? | - |
? | |
| UDP-glucuronate + naproxen | - |
Homo sapiens | ? | - |
? | |
| UDP-glucuronate + naproxen | UGT2B7 is responsible for human hepatic naproxen acyl glucuronidation, which is the primary elimination pathway for this drug | Homo sapiens | ? | - |
? | |
| UDPglucuronate + naproxen | UGT2B7 is responsible for human hepatic naproxen acyl glucuronidation, which is the primary elimination pathway for this drug | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| DP-glucuronosyltransferase 1A3 | - |
Homo sapiens |
| UDPGT | - |
Homo sapiens |
| UGT1-03 | - |
Homo sapiens |
| UGT1.3 | - |
Homo sapiens |
| UGT1A1 | - |
Homo sapiens |
| UGT1A3 | - |
Homo sapiens |
| UGT1A6 | - |
Homo sapiens |
| UGT1A7 | - |
Homo sapiens |
| UGT1A8 | - |
Homo sapiens |
| UGT1A9 | - |
Homo sapiens |
| UGT2B7 | - |
Homo sapiens |
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