Cancer chemotherapy is the treatment method which uses drugs to kill cancer cells or to inhibit their growth. In cancer drug discovery or development, not only anti-cancer drug delivery into target cancer cells across the cell membrane but also acquired anti-cancer drug resistance through the overexpression of ATP-binding cassette (ABC) transporters such as MDR1 (p-glycoprotein) in target cancer cells are serious problems to overcome. However, the use of transport system based on solute carrier (SLC) transporters can solve both problems, because it is well-known that some types of SLC transporters are overexpressed in cancer cells. Thus, transporter-consciously designed drugs can be transported into cells by such overexpressed SLC transporters, so as not to be excreted by MDR1. Therefore, transporter-conscious drug design is very effective in absorption, distribution, excretion, and toxicity of drugs (ADMET) due to transport systems. In this paper, cancer chemotherapy based on transporter-conscious drug design is described.
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