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Role of Transporters
 
Slide 21 of 22
 
Speaker notes: There are a whole range of molecules (P-glycoprotein and multi-drug resistant proteins) present in cells and tissues.

This has been recognised in the study of anticancer agents for a long time, and the implications of such mechanisms for antiretrovirals are now being more widely considered.

Transport proteins potentially limit how a drug enters cells:
  • Left-hand diagram: the drug can enter easily, and is not being actively effluxed
  • Right-hand diagram: efflux transporters are pushing drug out of the cells, reducing intracellular concentrations to below adequate levels for viral inhibition.
Although the major focus is currently on measurement of plasma levels of antiretrovirals, intracellular kinetics deserve more thorough consideration:
  • this issue needs to be studied in depth.

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