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

BRENDA support

Literature summary for 2.8.2.1 extracted from

  • Jia, C.; Luo, L.; Kurogi, K.; Yu, J.; Zhou, C.; Liu, M.-C.
    Identification of the human SULT enzymes involved in the metabolism of rotigotine (2016), J. Clin. Pharmacol., 56, 754-760 .
    View publication on PubMed
Search for more literature for 2.8.2.1

Application

Application Comment Organism
medicine isoforms SULT1A1, 1A2, 1A3, 1B1, 1C4, 1E1 display significant sulfating activities toward rotigotine. Of the 6 human organ samples tested, small intestine and liver cytosols display considerably higher rotigotine-sulfating activity than brain, lung, and kidney. Sulfation of rotigotine occurs in HepG2 cells and Caco-2 cells under metabolic conditions Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0291
-
 rotigotine pH 7.0, 37°C Homo sapiens
0.0313
-
 rotigotine pH 7.0, 37°C Homo sapiens
0.0807
-
 rotigotine pH 7.0, 37°C Homo sapiens
0.1191
-
 rotigotine pH 7.0, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O75897 isoform SULT1C4
-
Homo sapiens P0DMM9 isoform SULT1A3
-
Homo sapiens P50225 isoform SULT1A1
-
Homo sapiens P50226 isoform SULT1A2
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
6.4
-
 pH 7.0, 37°C Homo sapiens
11.8
-
 pH 7.0, 37°C Homo sapiens
14.2
-
 pH 7.0, 37°C Homo sapiens
29.1
-
 pH 7.0, 37°C Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3'-phosphoadenylyl sulfate + rotigotine i.e. (6S)-6-[propyl[2-(thiophen-2-yl)ethyl]amino]-5,6,7,8-tetrahydronaphthalen-1-ol, non-ergoline dopamine agonist Homo sapiens adenosine 3',5'-bisphosphate + rotigotine 1-O-sulfate
-
 ?

Synonyms

Synonyms Comment Organism
SULT1A1
-
 Homo sapiens
SULT1A2
-
 Homo sapiens
SULT1A3
-
 Homo sapiens
SULT1C4
-
 Homo sapiens