Druggable receptors

Set the task of discovering new, previously unknown druggable receptors, how would we go about it In particular, how would we find a GPCR The first step toward functional annotation of a new GPCR sequence usually involves searching a primary sequence database with pairwise similarity tools. Such searches can reveal clear similarities between the query sequence... 

Step 2 involves knowing what properties turn a macromolecule into a receptor. All receptors may be macromolecules, but all macromolecules are certainly not receptors. Receptor macromolecules are frequently proteins or glycoproteins. Certain properties must be present if a macromolecule is going to have what it takes to be a druggable target. The receptor macromolecule must be intimately connected with the disease in question, but not integral to the normal biochemistry of a wide range of processes. 

Most receptors and enzymes possess beautiful binding sites and, for this reason, are Ukely to remain a rich source of druggable targets. In contrast, many protein-protein interactions do not fulfill the above requirements and therefore represent hopeless drug targets. Because of their relevance to many diseases, however, protein-protein interactions are still attracting considerable interest and a few may ultimately turn out to be druggable. ... 

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