The Gatekeeper: Friend or Foe in Identifying the Next Generation of Kinase Inhibitors

Fighting cancer: The next generation of small‐molecule kinase inhibitors might be designed against distinct mutational forms of certain kinases. Current antitumor drugs display remarkable efficacy, but relapse is frequently observed during treatment due to acquired mutation. The gatekeeper plays an important role in this context, and compounds such as 1 that interact with it might be a starting point to design future inhibitors.