N Glycosamine

Figure 6.12 Structure of P-glycoprotein in the plasma membrane

It was soon realised that the wide diversity of compounds transported were mutual inhibitors, i.e. these compounds were also substrates for P-glycoprotein. Several of these reversal agents are now under trial in the treatment of acute myeloid leukaemia.

There is some speculation that P-glycoprotein may not prevent the complete absorption of a substrate but may simply control entry at a rate sufficient to ensure intestinal metabolism. The evidence for this is that the P-glycoprotein action appears to work in concert with cytochrome P450 3A4.

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