ABSTRACT

G protein-coupled receptors (GPCRs) and ion channels are expressed in the plasma membranes of virtually all cells. They usually serve as transmembrane signal transducers and/or transport proteins and are key regulators of cellular function. Following their activation, a cascade of downstream signaling events is triggered and this can lead to immediate and delayed effects on cell physiology and gene expression. The importance of the GPCR and ion channel families in the practice of medicine is reected in the myriad clinical drugs that target these proteins. GPCR and ion channel modulator drugs are used to treat major illnesses, including cardiovascular, metabolic, neurologic, and infectious diseases as well as some forms of cancer.