Draggable targets

Currently there are drugs for only a fraction of the draggable targets present in the human genome. 

The seven chapters of this volume describe recent progress towards drugs acting at a range of draggable targets. One chapter addresses kinases, one covers an ion channel, two feature proteases and three of the chapters cover G-protein coupled receptors, which have historically perhaps been the most fruitful area for medicinal chemists. 

Winum J-Y, Rami M, Scozzafava A, Montero J-L, Supuran C (2008) Carbonic anhydrase IX a new draggable target for the design of antitumor agents. Med Res Rev 28 445 -63... 

Voronkov M, Braithwaite SP, Stock JB (2011) Phosphoprotein phosphatase 2A a novel draggable target for Alzheimer s disease. Future Med Chem 3 821-833... 

The draggability of enzymes as targets reflects the evolution of enzyme structure to efficiently perform catalysis of chemical reactions, as discussed in the following section. 

P.J. Hajduk, J.R. Huth and S.W. Fesik, Draggability indices for protein targets derived from NMR-based screening data, J. Med. Chem., 48, 2518-2525 (2005). 

Another use of structures is in assessing a group of candidate target proteins to determine which is most likely to be draggable. By draggable, we mean that a molecule can be found that can be taken orally, will reach the target protein, and will have the desired effect with no side effects. While this question can only be decided definitively by experiment, examining structures to choose which experiments are most likely to succeed may save considerable time and expense. 

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