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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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The Sequencing Revolution: enabling personal genomics and personalised medicine

29 October 2010 | By Bhupinder Bhullar, Novartis Institute for Biomedical Research

It has been 10 years since the completion of the first draft of the human genome. Today, we are in the midst of a full assault on the human genetic code, racing to uncover the genetic mechanisms that affect disease, aging, happiness, violence ... and just about every imaginable human…

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Affinity-based screening

20 July 2006 | By Dr Lorenz M. Mayr, Executive Director & Head Biochemical Screening and Dr Hartmut Zehender, Labhead SpeedScreen, Biochemical Screening, Novartis Institute for Biomedical Research

Drug (lead) discovery relies on massive screening of chemical libraries against various extra- and intracellular molecular targets to find compounds with the desired mode of action. Sequencing of the human genome1 has generated a large number (>40 per cent) of new molecular targets with unknown function (‘orphan targets’), as well…

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Versatile miniaturised HTS

7 March 2005 | By Oliver Bruttger, Danielle Folio, Christine Niklaus and Johannes Ottl, Novartis Institute for BioMedical Research, Lead Discovery Center Basel

Research and development for a pharmaceutical company is a difficult and lengthy process. It stretches from the discovery phase to preclinical and clinical development stage, through the drug approval period ultimately to clinical application. The discovery research phase is one of the early key processes. The research starts with target…