ABSTRACT

Ion channels of the transient receptor potential melastatin (TRPM) subfamily are widely expressed in mammalian tissues and serve a diverse number of physiological roles, including temperature and taste sensation, insulin secretion, cardiovascular and neuronal function, and cancer, to name a few. The founding member of this family, TRPM1, was cloned in 1998, with an additional seven channels comprising this family that can be organized into subclasses based on sequence homology: TRPM1/TRPM3, TRPM2/TRPM8, TRPM4/TRPM5, TRPM7/TRPM7. However, in many cases these similarities in sequence and structure do not apply to the disparate function of these channels. Moreover, TRPM channels are unique in that some are bifunctional as both channels and enzymes. Recent elucidation of the structures of several TRPM channels has informed the gating mechanisms, pharmacology and assembly of these important proteins. This chapter reviews the molecular and functional properties of each family member providing insights into their roles in human diseases and their potential as therapeutic targets.