Discovery of potent, selective small molecule inhibitors of α-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIα)

  • Piotr Raubo, David M. Andrews, Jennifer C. McKelvie, Graeme R. Robb, James M. Smith, Martin E. Swarbrick, Michael J. Waring
  • Bioorganic & Medicinal Chemistry Letters, August 2015, Elsevier
  • DOI: 10.1016/j.bmcl.2015.05.093

PI4 Kinase Inhibitors

What is it about?

PI4 Kinase alpha is a biological target that has been implicated in both cancer and infection. Here we describe the discovery and optimisation of a very selective series of inhibitors

Why is it important?

Other inhibitors of this target have also been described. This series of inhibitors is very selective against the alpha form of the enzyme. Having access to a number of different chemical types of inhibitors should help biologists to unravel the precise cellular pathways that PI4 kinase effects

Perspectives

Dr David M Andrews
AstraZeneca Pharmaceutical Co Ltd

This work was done in collaboration with Cancer Research Technology - a great group to work with. It illustrates the benefits of working collaboratively: Working together revealed different insights and different skills; we were able to work on a target that either team on its own might have considered too high risk; the resulting tools should help biologists develop deeper understanding of the role (if any) of PI4 kinase in cancer.

Read Publication

http://dx.doi.org/10.1016/j.bmcl.2015.05.093

The following have contributed to this page: Dr David M Andrews