Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(+)-longifolol | a tricyclic sesquiterpenol | Homo sapiens | |
beta-phenyllongifolol | highly selective for isozyme UGT2B7, the mode of inhibition is rapidly reversible and competitive, inhibitor is not glucuronidated by UGT2B7 or other hepatic UGTs | Homo sapiens | |
additional information | design of UGT inhibitors based on rational principles such as detailed structure-activity relationships, synthesis of twenty-four homochiral and epimeric longifolol derivatives and screening for UGT2B7 inhibitory potency, determination of the absolute configuration at the stereogenic center C1' by X-ray crystallography and 2D NMR spectroscopy, gHSQC, gNOESY, stereochemistry, overview, substrate-dependent and substrate-independent inhibition, overview | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
UDP-glucuronate + acceptor | Homo sapiens | - |
UDP + acceptor beta-glucuronoside | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P16662 | isozyme UGT2B7; isozyme UGT2B7 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | inhibitor beta-phenyllongifolol is not glucuronidated by UGT2B7 or other hepatic UGTs | Homo sapiens | ? | - |
? | |
UDP-D-glucuronate + acceptor | - |
Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + estriol | - |
Homo sapiens | UDP + estriol glucuronoside | - |
? | |
UDP-D-glucuronate + scopoletin | - |
Homo sapiens | UDP + scopoletin beta-D-glucuronoside | - |
? | |
UDP-glucuronate + acceptor | - |
Homo sapiens | UDP + acceptor beta-glucuronoside | - |
? |
Synonyms | Comment | Organism |
---|---|---|
UDP-glucuronosyltransferase 2B7 | - |
Homo sapiens |
UGT2B7 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00000091 | - |
beta-phenyllongifolol | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
additional information | - |
inhibition of isozyme UGT2B7 at several different concentration of inhibitor compounds | Homo sapiens | additional information |