Type II kinase inhibitors: an opportunity in cancer for rational design
Javier Blanc, Raphaël Geney and Christel Menet
AbstractSince the introduction of the Type II kinase inhibitor imatinib (Gleevec) for treatment against cancer, rational design of tailored molecules has increased the opportunities in medicinal chemistry to tackle tumours related to kinase dysfunctionalities. Among the different types of kinase inhibitors, the design of Type II inhibitors has been rationalized to exploit the benefits and reduce the drawbacks. Here we present the advances with Type II inhibitors, discussing the advantages and disadvantages of these type of molecules. Moreover, we expose the strategies in designing druggable molecules that either selectively inhibit target kinases or overcome drug resistance.
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