Bpb

Ubiquitous (kidney, BCSFB, BTB)

Detoxification of xenobiotics?

Leukotriene (LTC4) secretion from leukocyte

Liver Kidney Intestine BPB

Liver Kidney

Excretion of bilirubin glucuronide and GSH into bile

Characteristics: Neutral or cationic compounds with bulky structure

Anticancer drugs: etoposide, doxorubicin, vincristine Ca2+ channel blockers: diltiazem, verapamil HIV protease inhibitors: indinavir, ritonavir Antibiotics/antifungals: erythromycin, ketoconazole Hormones: testosterone, progesterone Immunosuppressants: cyclosporine, FK506 (tacrolimus) Others: digoxin, quinidine

Characteristics: Amphiphilic with at least one negative net charge Anticancer drugs: vincristine (with GSH), methotrexate Glutathione conjugates: LTC4, glutathione conjugate of ethacrynic acid Glucuronide conjugates: estradiol-17-D-glucuronide, bilirubin mono(or bis) glucuronide

Sulfated conjugates: estrone-3-sulfate (with GSH) HIV protease inhibitors: saquinavir Antifungals: grepafloxacin Others: folate, GSH, oxidized glutathione

Characteristics: Amphiphilic with at least one negative net charge (similar to MRP1)

Anticancer drugs: methotrexate, vincristine Glutathione conjugates: LTC4, GSH conjugate of ethacrynic acid Glucuronide conjugates: estradiol-17-D-glucuronide, bilirubin mono(or bis) glucuronide

Sulfate conjugate of bile salts: taurolithocholate sulfate HIV protease inhibitors: indinavir, ritonavir Others: pravastatin, GSH, oxidized glutathione Characteristics: Amphiphilic with at least one negative net charge (Glucuronide conjugates are better substrates than glutathione conjugates.)

Intestine

MRP4 (ABCC4)

MRP5 (ABCC5)

MRP6 (ABCC6)

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