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Novartis collaboration aims to eliminate rheumatic heart disease (RHD) in Zambia

Industry news, News / 28 February 2013 / Novartis

Novartis today announced that it has launched an effort to eliminate rheumatic heart disease in Zambia in collaboration with the Lusaka…

Conformational Bias: A key concept for protein kinase inhibition

Drug Targets, Issue 1 2012 / 28 February 2012 / 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: an on state with maximal kinase activity (active kinase) and an off state with minimal activity on the other extreme. Conformational bias, i.e. a shift in the equilibrium between active and inactive conformations is a key determinant in kinase regulation and can be brought about by many factors including post-translational modifications, regulatory proteins, ligand binding etc. Kinase inhibitors can be viewed as particular ligands to protein kinases. As the mode of action is linked to the binding mode, the selectivity as well as the kinetics of kinase inhibitors can often be rationalised based on the target conformation. Pathologic kinase deregulation often involves a shift towards the active conformation, leading to constitutive signalling. In this review, we discuss how mutations act as a conformational bias and depending on the mode of action can lead to activation of the protein kinase that can either result in resistance or contribute to the efficacy of kinase inhibitors. Deregulation of protein kinase activities by mutations and/or amplification are associated with a variety of pathologies ranging from cancer to inflammatory diseases, diabetes, infectious diseases and cardiovascular and metabolic disorders…

Figure 1 Advances in the development of sequencing technologies have resulted in an increase in data output with a dramatic decrease in cost. This graph compares calculated sequencing costs for one complete haploid human genome sequence (23 chromosomes, three billion bases) * estimated from literature ** marketing figures

The Sequencing Revolution: enabling personal genomics and personalised medicine

Genomics, Issue 5 2010 / 29 October 2010 / 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 variation. Advances in DNA sequencing technology have enabled individuals to have their own genomes sequenced rapidly, cheaply and in astonishing detail. The sequencing revolution is also changing the way the pharmaceutical industry develops, tests and targets new medicines.

Affinity-based screening

Issue 4 2006, Past issues / 20 July 2006 / 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 as a large number of molecular targets with known function albeit non-tractable by standard high-throughput screening (HTS) due to the particular requirements of plate-based assays in robotic screening systems (‘non-tractable targets’). Examples of the latter are targets with very fast kinetics, targets with multiple modes of function for the same polypeptide chain or targets where the substrate of a particular enzyme is not known.

Versatile miniaturised HTS

Issue 1 2005, Past issues / 7 March 2005 / 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 identification and validation. Assays are […]


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