Cloned (Comment) | Organism |
---|---|
expression in HEK-293 cell, using baculoviral system | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
homology modeling with estradiol 17-beta-D-glucuronide, cyclic guanosine monophosphate, methotrextae and folic acid as substrates | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
F368A | almost complete disruption of transport activity for all substrates tested | Homo sapiens |
F368W | F368W-mediated estradiol 17-beta-D-glucuronide transport is increased to 250% of wild type MRP4, whereas cyclic guanosine monophosphate transport is decreased to 24% , and methotrextae and folic acid transport is reduced to 5580% of wild type transport activity | Homo sapiens |
F368Y | F368Y-mediated cyclic guanosine monophosphate transport is increased to 160%, while transport of the other substrates is decreased by 2050% compared to wild type | Homo sapiens |
additional information | residues F368 and W995 do not play an important role in the initial binding of substrates | Homo sapiens |
R998K | almost complete disruption of transport activity for all substrates tested | Homo sapiens |
R998L | almost complete disruption of transport activity for all substrates tested | Homo sapiens |
R998S | almost complete disruption of transport activity for all substrates tested | Homo sapiens |
R998Y | almost complete disruption of transport activity for all substrates tested | Homo sapiens |
W995A | almost complete disruption of transport activity for all substrates tested | Homo sapiens |
W995F | significantly decreased transport of all substrates | Homo sapiens |
W995Y | significantly decreased transport of all substrates | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.013 | - |
estradiol 17-beta-D-glucuronide/in | mutant W995Y, pH 7.5, 37°C | Homo sapiens | |
0.017 | - |
estradiol 17-beta-D-glucuronide/in | wild-type, pH 7.5, 37°C | Homo sapiens | |
0.017 | - |
estradiol 17-beta-D-glucuronide/in | mutant F368W, pH 7.5, 37°C | Homo sapiens | |
0.031 | - |
estradiol 17-beta-D-glucuronide/in | mutant F368Y, pH 7.5, 37°C | Homo sapiens | |
0.054 | - |
estradiol 17-beta-D-glucuronide/in | mutant W995F, pH 7.5, 37°C | Homo sapiens | |
0.13 | - |
folic acid/in | mutant W995Y, pH 7.5, 37°C | Homo sapiens | |
0.15 | - |
folic acid/in | mutant W995F, pH 7.5, 37°C | Homo sapiens | |
0.16 | - |
folic acid/in | mutant F368W, pH 7.5, 37°C | Homo sapiens | |
0.17 | - |
estradiol 17-beta-D-glucuronide/in | wild-type, pH 7.5, 37°C | Homo sapiens | |
0.24 | - |
methotrexate/in | mutant F368W, pH 7.5, 37°C | Homo sapiens | |
0.25 | - |
methotrexate/in | wild-type, pH 7.5, 37°C | Homo sapiens | |
0.26 | - |
folic acid/in | mutant F368Y, pH 7.5, 37°C | Homo sapiens | |
0.3 | - |
methotrexate/in | mutant F368Y, pH 7.5, 37°C | Homo sapiens | |
0.35 | - |
methotrexate/in | mutant W995F, pH 7.5, 37°C | Homo sapiens | |
0.36 | - |
cyclic guanosine monophosphate/in | mutant W995F, pH 7.5, 37°C | Homo sapiens | |
0.39 | - |
methotrexate/in | mutant W995Y, pH 7.5, 37°C | Homo sapiens | |
0.48 | - |
cyclic guanosine monophosphate/in | mutant F368Y, pH 7.5, 37°C | Homo sapiens | |
0.63 | - |
cyclic guanosine monophosphate/in | wild-type, pH 7.5, 37°C | Homo sapiens | |
1.8 | - |
cyclic guanosine monophosphate/in | mutant W995Y, pH 7.5, 37°C | Homo sapiens | |
2 | - |
cyclic guanosine monophosphate/in | mutant F368W, pH 7.5, 37°C | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
270 | - |
wild-type, substrate methotrexate, pH 7.5, 37°C | Homo sapiens |
580 | - |
wild-type, substrate estradiol 17-beta-D-glucuronide, pH 7.5, 37°C | Homo sapiens |
650 | - |
wild-type, substrate folic acid, pH 7.5, 37°C | Homo sapiens |
3500 | - |
wild-type, substrate cyclic guanosine monophosphate, pH 7.5, 37°C | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + H2O + cyclic guanosine monophosphate/in | - |
Homo sapiens | ADP + phosphate + cyclic guanosine monophosphate/out | - |
? | |
ATP + H2O + estradiol 17-beta-D-glucuronide/in | - |
Homo sapiens | ADP + phosphate + estradiol 17-beta-D-glucuronide/out | - |
? | |
ATP + H2O + folic acid/in | - |
Homo sapiens | ADP + phosphate + folic acid/out | - |
? | |
ATP + H2O + methotrexate/in | - |
Homo sapiens | ADP + phosphate + methotrexate/out | - |
? |
Synonyms | Comment | Organism |
---|---|---|
ABCC4 | - |
Homo sapiens |
MRP4 | - |
Homo sapiens |