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Literature summary for 2.4.1.17 extracted from

  • Bichlmaier, I.; Finel, M.; Sippl, W.; Yli-Kauhaluoma, J.
    Stereochemical and steric control of the UDP-glucuronosyltransferase-catalyzed conjugation reaction: a rational approach for the design of inhibitors for the human UGT2B7 (2007), ChemMedChem, 2, 1730-1740.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of isozyme UGT2B7 as a His-tagged protein in baculovirus-infected insect cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
((2R)-2-hydroxy-2-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethyl)phosphonic acid
-
Homo sapiens
((2S)-2-hydroxy-2-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethyl)phosphonic acid
-
Homo sapiens
((3R)-3-hydroxy-3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propyl)phosphonic acid
-
Homo sapiens
((3S)-3-hydroxy-3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propyl)phosphonic acid
-
Homo sapiens
(1R)-1-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]but-3-en-1-ol
-
Homo sapiens
(1R)-1-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethanol
-
Homo sapiens
(1R)-1-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]prop-2-en-1-ol
-
Homo sapiens
(1R)-1-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-1-ol
-
Homo sapiens
(1R)-1-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propane-1,3-diol
-
Homo sapiens
(1R)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]but-3-en-1-ol
-
Homo sapiens
(1R)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethan
-
Homo sapiens
(1R)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]prop-2-en-1-ol
-
Homo sapiens
(1R)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-1-ol
-
Homo sapiens
(1R)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propane-1,3-diol
-
Homo sapiens
(1R)-2,2-dimethyl-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-1-ol
-
Homo sapiens
(1R)-2-chloro-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethanol
-
Homo sapiens
(1R)-2-methyl-1-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-1-ol
-
Homo sapiens
(1R)-2-methyl-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-1-ol
-
Homo sapiens
(1S)-1-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propane-1,3-diol
-
Homo sapiens
(1S)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]but-3-en-1-ol
-
Homo sapiens
(1S)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethanol
-
Homo sapiens
(1S)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]prop-2-en-1-ol
-
Homo sapiens
(1S)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-1-ol
-
Homo sapiens
(1S)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propane-1,3-diol
-
Homo sapiens
(1S)-2,2-dimethyl-1-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-1-ol
-
Homo sapiens
(1S)-2,2-dimethyl-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-1-ol
-
Homo sapiens
(1S)-2-chloro-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethanol
-
Homo sapiens
(1S)-2-methyl-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-1-ol
-
Homo sapiens
(2-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethyl)phosphonic acid
-
Homo sapiens
(2E)-3-(4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl)prop-2-en-1-ol
-
Homo sapiens
(2E)-3-(4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl)prop-2-enoic acid
-
Homo sapiens
(2R)-3,3-dimethyl-2-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]butan-2-ol
-
Homo sapiens
(2S)-2-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]but-3-en-2-ol
-
Homo sapiens
(2S)-2-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]butan-2-ol
-
Homo sapiens
(2S)-2-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]pent-4-en-2-ol
-
Homo sapiens
(2S)-3-methyl-2-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]butan-2-ol
-
Homo sapiens
(2Z)-3-(4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl)prop-2-en-1-ol
-
Homo sapiens
(2Z)-3-(4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl)prop-2-enoic acid
-
Homo sapiens
(3-(dimethylamino)-1-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propyl)phosphonic acid
-
Homo sapiens
(3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propyl)phosphonic acid
-
Homo sapiens
(3R)-3-hydroxy-3-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propanoic acid
-
Homo sapiens
(3R)-3-hydroxy-3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propanoic acid
-
Homo sapiens
(3S)-3-hydroxy-3-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propanoic acid
-
Homo sapiens
(3S)-3-hydroxy-3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propanoic acid
-
Homo sapiens
(4-(dimethylamino)-2-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]butyl)phosphonic acid
-
Homo sapiens
(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulene-9-carboxylic acid
-
Homo sapiens
(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulene-9-carboxylic acid
-
Homo sapiens
(R)-phenyl[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]methanol
-
Homo sapiens
(S)-phenyl[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]methanol
-
Homo sapiens
(S)-phenyl[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]methanol
-
Homo sapiens
2-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethanol
-
Homo sapiens
2-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-2-ol
-
Homo sapiens
2-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethanol
-
Homo sapiens
3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propan-1-ol
-
Homo sapiens
4-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]butan-1-ol
-
Homo sapiens
4-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]butanoic acid
-
Homo sapiens
4-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]butan-1-ol
-
Homo sapiens
4-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]butanoic acid
-
Homo sapiens
diethyl ((2R)-2-hydroxy-2-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethyl)phosphonate
-
Homo sapiens
diethyl ((2S)-2-hydroxy-2-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]ethyl)phosphonate
-
Homo sapiens
diethyl ((3R)-3-hydroxy-3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propyl)phosphonate
-
Homo sapiens
diethyl ((3S)-3-hydroxy-3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propyl)phosphonate
-
Homo sapiens
dimethyl ((3R)-3-hydroxy-3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propyl)phosphonate
-
Homo sapiens
dimethyl ((3S)-3-hydroxy-3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propyl)phosphonate
-
Homo sapiens
ethyl (3R)-3-hydroxy-3-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propanoate
-
Homo sapiens
ethyl (3R)-3-hydroxy-3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propanoate
-
Homo sapiens
ethyl (3S)-3-hydroxy-3-[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propanoate
-
Homo sapiens
ethyl (3S)-3-hydroxy-3-[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]propanoate
-
Homo sapiens
isolongifolol and derivatives of primary alcohol series or carboxylic/phosphonic acids and amines, inhibitory potency, overview Homo sapiens
longifolol and derivatives of primary alcohol series or carboxylic/phosphonic acids and amines, inhibitory potency, overview Homo sapiens
additional information detailed structure-activity relationships, the glucuronidation of substrate compounds is prevented by the introduction of bulky substituents such as isopropyl, tert-butyl, and phenyl groups, overview Homo sapiens
[(1E)-3-(4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl)prop-1-en-1-yl]phosphonic acid
-
Homo sapiens
[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]acetic acid
-
Homo sapiens
[(9R)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]methanol
-
Homo sapiens
[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]acetic acid
-
Homo sapiens
[(9S)-4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl]methanol
-
Homo sapiens
[(E)-2-(4,8,8-trimethyldecahydro-1,4-methanoazulen-9-yl)ethenyl]phosphonic acid
-
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-D-glucuronate + acceptor Homo sapiens
-
UDP + acceptor beta-D-glucuronoside
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozyme UGT2B7
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information detailed structure-activity relationships with respect to functionality, stereochemical properties, and steric features, with 3D-quantitative structure-activity relationship using comparative molecular similarity analysis, overview. The glucuronidation of substrate compounds is prevented by the introduction of bulky substituents such as isopropyl, tert-butyl, and phenyl groups, overview Homo sapiens ?
-
?
UDP-D-glucuronate + acceptor
-
Homo sapiens UDP + acceptor beta-D-glucuronoside
-
?
UDP-D-glucuronate + estriol
-
Homo sapiens UDP + ?
-
?
UDP-D-glucuronate + isolongifolol the compound is substrate and competitive inhibitor Homo sapiens UDP + isolongifolol beta-D-glucuronoside
-
?
UDP-D-glucuronate + longifolol the compound is substrate and competitive inhibitor Homo sapiens UDP + longifolol beta-D-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
0.000023
-
isolongifolol
-
Homo sapiens
0.000026
-
longifolol
-
Homo sapiens