Fatty acids have long been known as important metabolic substrates and as structural components of biological membranes. However, they also function as signaling molecules. Recently, a series of G protein-coupled receptors (GPRs) for FAs has been described and characterized. Fatty acid receptors have been found to be expressed on different cell types and may be highly relevant to a number of metabolic related processes and diseases. For example, expression profiling indicates a wide range of fatty acid receptors within GI tract, immune cells, adipose tissue, pancreas and CNS. This meeting is an opportunity to raise and discuss in an open forum some of the challenges associated with understanding the pharmacology of this receptor family.