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Literature summary for 2.4.1.17 extracted from
- Inhibition of human UDP-glucuronosyltransferase enzymes by lapatinib, pazopanib, regorafenib and sorafenib Implications for hyperbilirubinemia (2017), Biochem. Pharmacol., 129, 85-95 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in HEK-293 cells | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| lapatinib | - |
Homo sapiens |  |
| additional information | isoforms UGT2B4, UGT2B7, UGT2B15 and UGT2B17 are not inhibited by lapatinib. Isoforms UGT2B4 and UGT2B17 are not inhibited by pazopanib. Isoforms UGT2B4 and UGT2B15 are not inhibited by regorafenib | Homo sapiens | |
| pazopanib | - |
Homo sapiens | |
| regorafenib | - |
Homo sapiens | |
| sorafenib | - |
Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Homo sapiens | - |
- |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | 4 mM used in assay conditions | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 4-methylumbelliferone + UDP-glucuronate | - |
Homo sapiens | UDP + 4-methylumbelliferyl-beta-D-glucuronide | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| UDP-glucuronosyltransferase | - |
Homo sapiens |
| UGT 1A10 | isoform | Homo sapiens |
| UGT 1A3 | isoform | Homo sapiens |
| UGT 1A4 | isoform | Homo sapiens |
| UGT 1A6 | isoform | Homo sapiens |
| UGT 1A7 | isoform | Homo sapiens |
| UGT 1A8 | isoform | Homo sapiens |
| UGT 1A9 | isoform | Homo sapiens |
| UGT 2B15 | isoform | Homo sapiens |
| UGT 2B17 | isoform | Homo sapiens |
| UGT 2B4 | isoform | Homo sapiens |
| UGT 2B7 | isoform | Homo sapiens |
| UGT1A1 | isoform | Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000045 | - |
isoform UGT1A1, at pH 7.4, temperature not specified in the publication | Homo sapiens | regorafenib | |
| 0.000066 | - |
isoform UGT1A1, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.000187 | - |
isoform UGT1A8, at pH 7.4, temperature not specified in the publication | Homo sapiens | pazopanib | |
| 0.000261 | - |
isoform UGT1A9, at pH 7.4, temperature not specified in the publication | Homo sapiens | regorafenib | |
| 0.000306 | - |
isoform UGT1A9, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.000317 | - |
isoform UGT1A7, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.000383 | - |
isoform UGT1A7, at pH 7.4, temperature not specified in the publication | Homo sapiens | regorafenib | |
| 0.000536 | - |
isoform UGT1A1, at pH 7.4, temperature not specified in the publication | Homo sapiens | lapatinib | |
| 0.000805 | - |
isoform UGT1A7, at pH 7.4, temperature not specified in the publication | Homo sapiens | pazopanib | |
| 0.0011 | - |
isoform UGT1A1, at pH 7.4, temperature not specified in the publication | Homo sapiens | pazopanib | |
| 0.0011 | - |
isoform UGT1A7, at pH 7.4, temperature not specified in the publication | Homo sapiens | lapatinib | |
| 0.0011 | - |
isoform UGT1A9, at pH 7.4, temperature not specified in the publication | Homo sapiens | lapatinib | |
| 0.0015 | - |
isoform UGT1A8, at pH 7.4, temperature not specified in the publication | Homo sapiens | lapatinib | |
| 0.00159 | - |
isoform UGT1A8, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.002 | - |
isoform UGT1A9, at pH 7.4, temperature not specified in the publication | Homo sapiens | pazopanib | |
| 0.0023 | - |
isoform UGT1A3, at pH 7.4, temperature not specified in the publication | Homo sapiens | lapatinib | |
| 0.0034 | - |
isoform UGT1A6, at pH 7.4, temperature not specified in the publication | Homo sapiens | lapatinib | |
| 0.0035 | - |
isoform UGT1A6, at pH 7.4, temperature not specified in the publication | Homo sapiens | pazopanib | |
| 0.0039 | - |
isoform UGT1A6, at pH 7.4, temperature not specified in the publication | Homo sapiens | regorafenib | |
| 0.0042 | - |
isoform UGT1A6, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.0052 | - |
isoform UGT1A8, at pH 7.4, temperature not specified in the publication | Homo sapiens | regorafenib | |
| 0.0075 | - |
isoform UGT1A10, at pH 7.4, temperature not specified in the publication | Homo sapiens | pazopanib | |
| 0.0076 | - |
isoform UGT1A10, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.0082 | - |
isoform UGT1A10, at pH 7.4, temperature not specified in the publication | Homo sapiens | lapatinib | |
| 0.0085 | - |
isoform UGT1A10, at pH 7.4, temperature not specified in the publication | Homo sapiens | regorafenib | |
| 0.0092 | - |
isoform UGT1A4, at pH 7.4, temperature not specified in the publication | Homo sapiens | lapatinib | |
| 0.0113 | - |
isoform UGT1A4, at pH 7.4, temperature not specified in the publication | Homo sapiens | pazopanib | |
| 0.016 | - |
isoform UGT1A4, at pH 7.4, temperature not specified in the publication | Homo sapiens | regorafenib | |
| 0.0161 | - |
isoform UGT1A4, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.0193 | - |
isoform UGT1A3, at pH 7.4, temperature not specified in the publication | Homo sapiens | regorafenib | |
| 0.0198 | - |
isoform UGT2B7, at pH 7.4, temperature not specified in the publication | Homo sapiens | pazopanib | |
| 0.0215 | - |
isoform UGT2B17, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.0273 | - |
isoform UGT1A3, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.0355 | - |
isoform UGT1A3, at pH 7.4, temperature not specified in the publication | Homo sapiens | pazopanib | |
| 0.0391 | - |
isoform UGT2B17, at pH 7.4, temperature not specified in the publication | Homo sapiens | regorafenib | |
| 0.0442 | - |
isoform UGT2B15, at pH 7.4, temperature not specified in the publication | Homo sapiens | pazopanib | |
| 0.0522 | - |
isoform UGT2B7, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.0544 | - |
isoform UGT2B4, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.0587 | - |
isoform UGT2B15, at pH 7.4, temperature not specified in the publication | Homo sapiens | sorafenib | |
| 0.0655 | - |
isoform UGT2B7, at pH 7.4, temperature not specified in the publication | Homo sapiens | regorafenib | |
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