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Literature summary for 2.4.1.17 extracted from

  • Sneitz, N.; Krishnan, K.; Covey, D.F.; Finel, M.
    Glucuronidation of the steroid enantiomers ent-17beta-estradiol, ent-androsterone and ent-etiocholanolone by the human UDP-glucuronosyltransferases (2011), J. Steroid Biochem. Mol. Biol., 127, 282-288.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
17beta-estradiol
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0143
-
17beta-estradiol isoform UGT1A10, pH 7.4, 37°C Homo sapiens
0.0297
-
17beta-estradiol isoform UGT2B7, pH 7.4, 37°C Homo sapiens
0.0975
-
17beta-estradiol isoform UGT2A1, pH 7.4, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
17alpha-estradiol + UDP-alpha-D-glucuronate
-
Homo sapiens ? + UDP
-
?
17beta-estradiol + UDP-alpha-D-glucuronate
-
Homo sapiens ? + UDP
-
?
additional information the pattern of human UDP-glucuronosyltransferases of subfamily 2B that glucuronidate ent-17beta-estradiol, particularly 2B15 and 2B17, resembles the glucuronidation of 17alpha-estradiol rather than 17beta-estradiol. The UDP-glucuronosyltransferases of subfamilies 1A and 2A exhibit higher degree of regioselectivity than enantioselectivity in the conjugation of these estradiols, regardless of whether the activity is primarily toward the non-chiral site, 3-OH, or the 17-OH group Homo sapiens ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.533
-
17beta-estradiol isoform UGT2B7, pH 7.4, 37°C Homo sapiens
1.547
-
17beta-estradiol isoform UGT1A10, pH 7.4, 37°C Homo sapiens