Ubiquitous (kidney, BCSFB, BTB)
Detoxification of xenobiotics?
Leukotriene (LTC4) secretion from leukocyte
Liver Kidney Intestine BPB
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.)
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