The g protein coupled receptor gpcr superfamily consists of structurally similar proteins arranged into families classes and is one of the most abundant protein classes in the mammalian genome 1 5 gpcrs undertake a plethora of essential physiological functions and are targets for numerous novel drugs 45 their ligands are structurally heterogenous including natural odorants nucleotides amines peptides proteins and lipids 4 the conserved structure of gpcrs consists of seven . G protein coupled receptors structure and function in drug discovery chiemela s odoemelam a benita percival a helen wallisa ming wei changb zeeshan ahmadc dawn scholeya emily burtona ian h williams d caroline lynn kamerlin e and philippe b wilson a the g protein coupled receptors gpcrs superfamily comprise similar proteins arranged into families or. G protein coupled receptors gpcrs are the largest family of cell surface receptors with more than 800 members identified thus far in the human genome they regulate the function of most cells in the body and represent approximately 3 of the genes in the human genome these receptors respond to a wide variety of structurally diverse ligands ranging from small molecules such as biogenic amines nucleotides and ions to lipids peptides proteins and even light ligands agonists and . As one of the most successful therapeutic target families g protein coupled receptors gpcrs have experienced a transformation from random ligand screening to knowledge driven drug design we are eye witnessing tremendous progresses made recently in the understanding of their structure function relationships that facilitated drug development at an unprecedented pace this article intends to provide a comprehensive overview of this important field to a broader readership that shares some . G protein coupled receptors from structure to function edited by jesus giraldo and jean philippe pin g protein coupled receptors regulate the function of most cells in the human body and represent approximately three percent of the genes in the human genome these receptors respond to a wide variety of structurally diverse ligands ranging from small molecules to lipids peptides proteins