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Literature summary for 7.6.2.2 extracted from

  • Sato, T.; Kodan, A.; Kimura, Y.; Ueda, K.; Nakatsu, T.; Kato, H.
    Functional role of the linker region in purified human P-glycoprotein (2009), FEBS J., 276, 3504-3516.
    View publication on PubMed
Search for more literature for 7.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
wild-type human P-gp is expressed using the baculovirus/expressSF+ insect cell system Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.000383
-
 nicardipine/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
0.000614
-
 verapamil/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
0.000637
-
 verapamil/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
0.000652
-
 nicardipine/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
0.000665
-
 paclitaxel/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
0.000775
-
 paclitaxel/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
0.000874
-
 paclitaxel/in pH 7.4, 37°C, native enzyme Homo sapiens
0.00121
-
 vinblastine/in pH 7.4, 37°C, native enzyme Homo sapiens
0.00191
-
 nicardipine/in pH 7.4, 37°C, native enzyme Homo sapiens
0.00201
-
 vinblastine/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
0.00236
-
 vinblastine/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
0.00423
-
 verapamil/in pH 7.4, 37°C, native enzyme Homo sapiens
0.0109
-
 rhodamine B/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
0.0118
-
 rhodamine 123/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
0.0142
-
 rhodamine B/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
0.0175
-
 rhodamine 123/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
0.0298
-
 rhodamine B/in pH 7.4, 37°C, native enzyme Homo sapiens
0.0354
-
 rhodamine 123/in pH 7.4, 37°C, native enzyme Homo sapiens
0.101
-
 digoxin/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
0.119
-
 digoxin/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
0.187
-
 digoxin/in pH 7.4, 37°C, native enzyme Homo sapiens
0.278
-
 colchicine/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
0.28
-
 colchicine/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
0.59
-
 ATP pH 7.4, 37°C, native enzyme Homo sapiens
0.72
-
 colchicine/in pH 7.4, 37°C, native enzyme Homo sapiens
0.89
-
 ATP pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane P-gp possesses a linker region of about 75 amino acids that connects two homologous halves, each of which contain a transmembrane domain followed by a nucleotide-binding domain Homo sapiens 16020
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + colchicine/in
-
 Homo sapiens ADP + phosphate + colchicine/out
-
 ?
ATP + H2O + digoxin/in
-
 Homo sapiens ADP + phosphate + digoxin/out
-
 ?
ATP + H2O + nicardipine/in
-
 Homo sapiens ADP + phosphate + nicardipine/out
-
 ?
ATP + H2O + paclitaxel/in
-
 Homo sapiens ADP + phosphate + paclitaxel/out
-
 ?
ATP + H2O + rhodamine 123/in
-
 Homo sapiens ADP + phosphate + rhodamine 123/out
-
 ?
ATP + H2O + rhodamine B/in
-
 Homo sapiens ADP + phosphate + rhodamine B/out
-
 ?
ATP + H2O + verapamil/in
-
 Homo sapiens ADP + phosphate + verapamil/out
-
 ?
ATP + H2O + vinblastine/in
-
 Homo sapiens ADP + phosphate + vinblastine/out
-
 ?
additional information P-gp possesses a linker region of about 75 amino acids that connects two homologous halves, each of which contain a transmembrane domain followed by a nucleotide-binding domain. The linker region regulates the inherent substrate specificity of P-gp Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
P-glycoprotein
-
 Homo sapiens

Temperature Stability [°C]

Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
additional information
-
 no effect of trypsin cleavage on the thermostability of P-gp Homo sapiens
40
-
 20 min, about 30% loss of activity Homo sapiens
45
-
 5 min, about 40% loss of activity Homo sapiens
50
-
 5 min, 5 min, about 90% of activity Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.189
-
 ATP pH 7.4, 37°C, native enzyme, value for basal ATPase activity with no transport substrate Homo sapiens
0.791
-
 digoxin/in pH 7.4, 37°C, native enzyme Homo sapiens
1.25
-
 colchicine/in pH 7.4, 37°C, native enzyme Homo sapiens
1.3
-
 paclitaxel/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
1.5
-
 paclitaxel/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
1.84
-
 rhodamine 123/in pH 7.4, 37°C, native enzyme Homo sapiens
1.9
-
 vinblastine/in pH 7.4, 37°C, native enzyme Homo sapiens
2.2
-
 paclitaxel/in pH 7.4, 37°C, native enzyme Homo sapiens
2.23
-
 rhodamine B/in pH 7.4, 37°C, native enzyme Homo sapiens
2.38
-
 ATP pH 7.4, 37°C, trypsin-cleaved enzyme, value for basal ATPase activity with no transport substrate Homo sapiens
2.95
-
 ATP pH 7.4, 37°C, chymotrypsin-cleaved enzyme, value for basal ATPase activity with no transport substrate Homo sapiens
3.28
-
 verapamil/in pH 7.4, 37°C, native enzyme Homo sapiens
3.48
-
 nicardipine/in pH 7.4, 37°C, native enzyme Homo sapiens
5.65
-
 digoxin/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
5.99
-
 digoxin/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
6.39
-
 vinblastine/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
6.4
-
 colchicine/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
6.54
-
 vinblastine/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
6.99
-
 rhodamine B/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
7.22
-
 rhodamine B/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
7.71
-
 verapamil/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
7.8
-
 nicardipine/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
7.81
-
 colchicine/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
8.19
-
 rhodamine 123/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
8.27
-
 verapamil/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
8.44
-
 nicardipine/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
8.56
-
 rhodamine 123/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens

General Information

General Information Comment Organism
physiological function P-glycoprotein conveys multidrug resistance. It is an ATP-dependent drug efflux pump that transports a wide variety of structurally unrelated compounds out of cells Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1.66
-
 colchicine/in pH 7.4, 37°C, native enzyme Homo sapiens
4.23
-
 digoxin/in pH 7.4, 37°C, native enzyme Homo sapiens
22.9
-
 colchicine/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
28.2
-
 colchicine/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
47.3
-
 digoxin/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
52
-
 rhodamine 123/in pH 7.4, 37°C, native enzyme Homo sapiens
59.2
-
 digoxin/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
74.9
-
 rhodamine B/in pH 7.4, 37°C, native enzyme Homo sapiens
469
-
 paclitaxel/in pH 7.4, 37°C, native enzyme Homo sapiens
489
-
 rhodamine 123/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
509
-
 rhodamine B/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
641
-
 rhodamine B/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
692
-
 rhodamine 123/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
775
-
 verapamil/in pH 7.4, 37°C, native enzyme Homo sapiens
1560
-
 vinblastine/in pH 7.4, 37°C, native enzyme Homo sapiens
1820
-
 nicardipine/in pH 7.4, 37°C, native enzyme Homo sapiens
2770
-
 vinblastine/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
3170
-
 vinblastine/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
4440
-
 paclitaxel/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
5630
-
 paclitaxel/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
12100
-
 verapamil/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens
12900
-
 nicardipine/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
13500
-
 verapamil/in pH 7.4, 37°C, trypsin-cleaved enzyme Homo sapiens
20400
-
 nicardipine/in pH 7.4, 37°C, chymotrypsin-cleaved enzyme Homo sapiens