Recent and new targets for small molecule anti-cancer agents

The first small molecules used for cancer treatment entered the clinic half a century ago, in the wake of antibiotic discoveries. Most drug targets in cancer therapy are shared with normal tissue, explaining the severe side effects of most anti-cancer drugs. Antifolates and anti-hormonal drugs, the first directed anti-cancer drugs that were developed, have entered the clinic only some few decades ago. More recently, small molecules have emerged that hit more specific tumor targets like BCR–Abl in CML. This also defined a new class of druggable enzymes: kinases which are now one of the most intensively studied targets by Pharma. Other novel protein classes such as proteasomes and PARP are also explored for their potential as anti-cancer targets. In parallel, novel combinations of established anti-cancer drugs are tested. Identifying novel drugs and drug combinations for cancer treatment is essential to transform a mortal into a more chronic disease.

Section editor:Peter Timmerman – Pepscan Therapeutics Zuidersluisweg 2, 8243 RC Lelystad, The Netherlands