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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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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:…

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UV-Vis scan-based quality control of assay-ready plates for improved data integrity

19 April 2011 | By Gary K Smith, M Anthony Leesnitzer, Lois L Wright, Iona Popa-Burke, Trevor Casserly, Luke Miller, Melissa Gomez & Iris Scherer, GlaxoSmithKline

Quality biological data requires both a high quality assay and a high quality compound. While assay quality is very closely monitored and has been intensively studied in the past, the quality of the final compound solutions being tested in an assay has received little attention. Quality of these samples is…