ATP-competitive choline kinase inhibitors to fight cancer

For a long time, protein kinases have  represented an attractive target in oncology drug discovery. However, it is often difficult to find selective agents as the ATP binding pocket is highly conserved.

Choline kinase (ChoK) is the enzyme responsible for the synthesis of phosphocholine (PCho). An increase of PCho molecules within the body can signify tumour progression, so ChoK is considered a promising drug target for cancer therapy. 

In this study, scientists at Nerviano Medical Sciences used Macromolecular Crystallography (MX) to identify selective and effective ATP-competitive compounds to inhibit ChoK.

Read the publication to find out more.

^{Image: Medical oncology services by Nick Youngson CC BY-SA 3.0 Pix4free}