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Literature summary extracted from

  • Bichlmaier, I.; Kurkela, M.; Joshi, T.; Siiskonen, A.; Rueffer, T.; Lang, H.; Finel, M.; Yli-Kauhaluoma, J.
    Potent inhibitors of the human UDP-glucuronosyltransferase 2B7 derived from the sesquiterpenoid alcohol longifolol (2007), ChemMedChem, 2, 881-889.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 (+)-longifolol a tricyclic sesquiterpenol Homo sapiens
2.4.1.17 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
2.4.1.17 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

EC Number Localization Comment Organism GeneOntology No. Textmining
2.4.1.17 microsome
-
 Homo sapiens
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.4.1.17 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.1.17 UDP-glucuronate + acceptor Homo sapiens
-
 UDP + acceptor beta-glucuronoside
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens P16662 isozyme UGT2B7; isozyme UGT2B7
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.17 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 additional information inhibitor beta-phenyllongifolol is not glucuronidated by UGT2B7 or other hepatic UGTs Homo sapiens ?
-
 ?
2.4.1.17 UDP-D-glucuronate + acceptor
-
 Homo sapiens UDP + acceptor beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + estriol
-
 Homo sapiens UDP + estriol glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + scopoletin
-
 Homo sapiens UDP + scopoletin beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-glucuronate + acceptor
-
 Homo sapiens UDP + acceptor beta-glucuronoside
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UDP-glucuronosyltransferase 2B7
-
 Homo sapiens
2.4.1.17 UGT2B7
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.1.17 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.1.17 7.4
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 0.00000091
-
 beta-phenyllongifolol
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.17 additional information
-
 inhibition of isozyme UGT2B7 at several different concentration of inhibitor compounds Homo sapiens additional information