Transporters are a kind of membrane proteins controlling uptake and efflux of essential nutrients ions, neurotransmitters, cellular waste, environmental toxins, and drugs, into and out of cells and organelles. Therefore, transporters play a significant important role in drug's clinical efficacy and safety. Currently, transporters are used as therapeutic targets to treat numerous diseases such as diabetes, asthma, cardiovascular diseases, major depression, neuroscience, hypertension and constipation.
In human genome, more than 400 membrane transporters are annotated. Generally, membrane transporters are divided into two major super-families, the ATP binding cassette (ABC) family and the solute carrier (SLC) family. Preclinical and clinical studies indicate that transport is an important determinant of drug disposition, as well as therapeutic and adverse drug effects.