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Can mTOR kinase inhibitors beat rapalogues in fighting against cancer?

19 February 2014 | By

The mammalian target of rapamycin (mTOR) has emerged as a promising cancer therapeutic target. Some rapamycin analogues (rapalogues) as mTOR allosteric inhibitors are FDA-approved drugs for treatment of certain types of cancers. However, the modest clinical anticancer activity of rapalogues, which preferentially inhibit mTOR complex 1, in most types of…

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Getting to grips with drug resistance in the human protein kinase superfamily

21 February 2013 | By Patrick A Eyers, Department of Oncology, Sheffield Cancer Research Centre, University of Sheffield

Protein kinases represent a vast, partially untapped resource of drug targets for therapeutic intervention in human disease. The remarkable success of the tyrosine kinase inhibitor Imatinib, which is now the first-line therapy in Philadelphia-positive tyrosine kinase inhibitor Imatinibhas galvanised biomedical researchers in an attempt to repeat the landmark success of…

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Conformational Bias: A key concept for protein kinase inhibition

28 February 2012 | By Henrik Möbitz, Global Discovery Chemistry, Computer Aided Drug Design, Novartis Institutes for Biomedical Research and Doriano Fabbro, Expertise Platform Kinases, Novartis Institutes for Biomedical Research

Protein kinases act as molecular switches with remarkable plasticity and dynamics upon interaction with specific regulatory domains as well as modulators. Conformation provides a conceptual framework for understanding many aspects of kinase biology. The kinase domain has precise structural prerequisites for signal transfer and can oscillate between two major conformations:…