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  GPCR and Disease Primer  

-protein-coupled receptors (GPCRs) are membrane embedded proteins that facilitate communication between the cell and its environment by passing chemical signals across the cell membrane to "second messenger" systems such as adenylate cyclase/cyclic AMP and phosphatidyl inositol (PIP2).

GPCRs comprise a large and functionally diverse superfamily of proteins that form a seven transmembrane helices bundle with alternating extracellular and intracellular loops. A very diverse range of ligands use this class of receptors to convert external and internal stimuli into intracellular responses (e.g., ions, biogenic amines, nucleosides, lipids, peptides, proteins, and even light).

GPCR receptors are involved in a wide variety of body systems and processes and control the physiology of almost all major organs in the body. Moreover, GPCRs are important in major diseases such as hypertension, cardiac dysfunction, depression, anxiety, obesity, inflammation and pain.

With the cloning of the human genome, it is now clear that over 800 human GPCRs exist. About half of these are involved in olfactory detection (smell and taste). Of the remaining 400, about 250 GPCRs are known to bind specific ligands. The remaining 150 GPCRs are known as orphan receptors, and represent a rich untapped area for novel discovery and drug development.