Biomedical Engineering Reference
In-Depth Information
TABLE 11.2. Substrates and Drug Resistance Profiles of Human ABCC/MRP
Transporters
Substrate
a
K
m
(
μ
M)
Refs.
Drug Resistance
b
Refs.
ABCC1
Leukotriene C
4
0.1
77,78,89
Doxorubicin
99,100
Leukotriene D
4
78,82
Daunorubicin
99
Leukotriene E
4
78,82
Epirubicin
99
N
-Acetyl leukotriene E
4
82
Vincristine
99,100
S
-Glutathionyl aflatoxin B1
0.2
87
Vinblastine
99
S
-Glutathionyl 2,4-dinitrobenzene
3.6
77,79,82
Etoposide
99
S
-Glutathionyl prostaglandin A
2
86
Arsenite
99
S
-Glutathionyl ethacrynic acid
28
85
Antimony
99
S
-Glutathionyl
N
-ethylmaleimide
101
Taxol
99
Chlorambucil
Colchicine
99
Monochloro monoglutathionyl
88
Monohydroxy monoglutathionyl
88
Bisglutathionyl
88
Melphalan
Monochloro monoglutathionyl
82,88
Monohydroxy monoglutathionyl
88
Glutathione disulfide (GSSG)
93
83
GSH (
+
verapamil)
c
83
92
Vincristine
+
GSH
d
89-91
Daunorubicin
+
GSH
d
91
Aflatoxin B1
+
GSH
d
87
Estrone 3-sulfate (
+
GSH)
c
0.7
95
Estrone 3-sulfate
4.2
95
β
-
O
-Glucuronosyl NNAL (
+
GSH)
c
39
96
Bilirubin
Monoglucuronosyl
102
Bisglucuronosyl
102
17
β
-Glucuronosyl estradiol
b1.5
82
2.5
84
6
α
-Glucuronosyl hyodeoxycholate
82
Glucuronosyl etoposide
82
Lithocholyltaurine 3-sulfate
82
Folate
76
Methotrexae
50
97
Fluo-3
12
103
p
-Aminohippurate
372
98
ABCC2
Leukotriene C
4
1
70
Cisplatin
70,108
S
-Glutathionyl 2,4-dinitrobenzene
6.5
105
Etoposide
70
S
-Glutathionyl ethacrynic acid
105
Vincristine
70
Bilirubin
Doxorubicin
70
Monoglucuronosyl
0.7
104
Epirubicin
70
Bisglucuronosyl
0.9
104
Methotrexate
97
(
Continued
)
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