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Priority Review granted to pemigatinib for treatment of cholangiocarcinoma
The US FDA has awarded pemigatinib Priority Review, after the drug met its primary and secondary endpoints in a Phase II trial.
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protein kinases
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Plasmonic biosensors enable development of new easy-to-use health tests
Researchers have developed a biosensor that can detect diseased exosomes, important indicators of various health conditions...
article
Can mTOR kinase inhibitors beat rapalogues in fighting against cancer?
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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Issue #4 2013 – Digital edition
Read the free digital version of the August / September edition of European Pharmaceutical Review magazine...
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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:…
