Alternative Splicing: Expanding Diversity in Major ABC and SLC Drug Transporters

Alternative splicing is an important mechanism of genetic regulation enhancing diversity and complexity of the transcriptome and proteome from the finite number of genes. Many reported cases demonstrate that alternative splicing events can lead to changes in the expression/function of proteins during disease development and progression. For pharmacogenes that can influence drug disposition and response, the role of alternative splicing has begun to receive increasing attention as an under-explored source of variable drug response. Here, we provide an overview of alternative spliced variants reported for the major drug transporters of SLC and ABC families with their possible implications in disease and drug therapy. As more comprehensive analyses on the abundance and functional outcomes of variably spliced isoforms of major drug transporters become available, it will be possible to utilize the obtained knowledge as novel therapeutic targets for tailored treatment strategies.