PCL102H1 Lecture Notes - Lecture 14: Multiple Drug Resistance
27 Apr 2016
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Document Summary
Substrates that get pumped out may have little structural (chemical) similarity to one another. P-glycoprotein is a type of pump that can transport a wide variety of structurally different drugs out of cells. Uses atp to pump drugs atp binding causes shape change of pump, allowing drug to leave. Strategies to prevent drugs from being pumped out of cells. General strategy for preventing drug efflux, not just drug of interest. Example using pgp inhibitor to improve therapeutic concentrations and therapeutic effect of cancer drug. Many cancer cells increase the amount of pgp pumps as a resistance mechanism to cancer drugs. When pgp is around at higher levels, it affects the efflux of drugs other than the drug that triggered the resistance mechanism. Also true for antiviral drugs (hiv) and antibiotics. Non-human organisms also have own drug pumps 5-10% of bacterial genes code for efflux pumps.
