Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.4.1.17 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
Search for more literature for 2.4.1.17

Inhibitors

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

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P16662 isozyme UGT2B7; isozyme UGT2B7
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
UDP-glucuronosyltransferase 2B7
-
 Homo sapiens
UGT2B7
-
 Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

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

Ki Value [mM]

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

IC50 Value

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