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Literature summary for 2.4.1.17 extracted from

  • Hanioka, N.; Hayashi, K.; Shimizudani, T.; Nagaoka, K.; Koeda, A.; Naito, S.; Narimatsu, S.
    Stereoselective glucuronidation of propranolol in human and cynomolgus monkey liver microsomes: role of human hepatic UDP-glucuronosyltransferase isoforms, UGT1A9, UGT2B4 and UGT2B7 (2008), Pharmacology, 82, 293-303.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in insect cell Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
hyodeoxycholic acid
-
Homo sapiens
propofol
-
Homo sapiens
zidovudine
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.135
-
(S)-propanolol isoform UGT1A9, pH 7.4, 37°C Homo sapiens
0.16
-
(R)-propanolol isoform UGT1A9, pH 7.4, 37°C Homo sapiens
0.263
-
(R)-propanolol isoform UGT2B7, pH 7.4, 37°C Homo sapiens
0.289
-
(S)-propanolol isoform UGT2B7, pH 7.4, 37°C Homo sapiens
0.515
-
(S)-propanolol isoform UGT2B4, pH 7.4, 37°C Homo sapiens
1.21
-
(R)-propanolol isoform UGT2B4, pH 7.4, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(R)-propanolol + UDP-glucuronate
-
Homo sapiens UDP + (R)-propanolol O-glucuronide
-
?
(S)-propanolol + UDP-glucuronate
-
Homo sapiens UDP + (S)-propanolol O-glucuronide
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0614
-
isoform UGT2B4, substrate (S)-propanolol, pH 7.4, 37°C Homo sapiens hyodeoxycholic acid
0.086
-
isoform UGT1A9, substrate (R)-propanolol, pH 7.4, 37°C Homo sapiens propofol
0.102
-
isoform UGT2B4, substrate (R)-propanolol, pH 7.4, 37°C Homo sapiens hyodeoxycholic acid
0.16
-
isoform UGT1A9, substrate (S)-propanolol, pH 7.4, 37°C Homo sapiens propofol
2.54
-
isoform UGT2B7, substrate (R)-propanolol, pH 7.4, 37°C Homo sapiens zidovudine
3.59
-
isoform UGT2B7, substrate (S)-propanolol, pH 7.4, 37°C Homo sapiens zidovudine