ABSTRACT

G protein-coupled receptors (GPCRs) are the largest protein family in the human genome. GPCRs are prevalent in all cell types, including airway smooth muscle (ASM). ASM represents an interesting cell type to the GPCR biologist because of the numerous different GPCRs they express, many being of physiological consequence. Cell-based models using ASM cultures derived from either humans or various animals represent arguably the most useful model for understanding GPCR expression and signaling in ASM. Refinement of culturing techniques for both human and non-human ASM cultures has produced a reliable system for studying ASM pharmacology, biology, physiology, and the roles of GPCRs in each of these disciplines. In vivo models provide the best models for testing the effects of GPCR ligands on airway resistance and, if human, the ultimate model for assessing utility of a GPCR ligand as lung disease therapeutic.