Content area
Full Text
R e s e a R c h h i g h l i g h t s
A N T I C A N C E R D R U G S
Redesigning kinase inhibitors
IMAGE SOURCE
The kinase inhibitor imatinib has been highly successful in the treatment of both chronic myelogenous leukaemia (CML) and gastrointestinal stromal tumours (GISTs); however, it has been associated with uncommon, but severe, cardiotoxicity.
Now, writing in JCI, Fernndezand colleagues describe their novel approach of re-engineering imatinib to alter its kinase inhibition profile to specifically target GISTs, while reducing its toxic effects on the heart.
Protein kinases are prime targets for anticancer therapies, but their close structural similarities can make achieving specificity for a particular kinase challenging, potentially leading to unwanted side effects. With...