This collection of cutting-edge methodologies for studying membrane transporters and channels takes advantage of all the latest developments in biomedical research, including pharmacogenomcs, bioinformatics, and microarray technologies. The authors explain databases and tools for bioinformatics studies, provide practical guidelines for microarray experiments and data analysis, and illustrate the use of small angle X-ray scattering, nuclear magnetic resonance (NMR), and molecular modeling to study the structural biology of membrane transporters. Methods for exploring structure–function correlation, such as site-directed mutagenesis, immunocytochemistry, and confocal microcopy are also described, along with several that may help in the development of novel therapeutics.