Comprehensive characterization of the Published Kinase Inhibitor Set

Despite the success of protein kinase inhibitors as approved therapeutics, drug discovery has focused on a small subset of kinase targets. Here we provide a thorough characterization of the Published Kinase Inhibitor Set (PKIS), a set of 367 small-molecule ATP-competitive kinase inhibitors that was recently made freely available with the aim of expanding research in this field and as an experiment in open-source target validation. We screen the set in activity assays with 224 recombinant kinases and 24 G protein-coupled receptors and in cellular assays of cancer cell proliferation and angiogenesis. We identify chemical starting points for designing new chemical probes of orphan kinases and illustrate the utility of these leads by developing a selective inhibitor for the previously untargeted kinases LOK and SLK. Our cellular screens reveal compounds that modulate cancer cell growth and angiogenesis in vitro. These reagents and associated data illustrate an efficient way forward to increasing understanding of the historically untargeted kinome

Science in Antarctica – a matter of quality

Antarctic research has progressed steadily from the era of reconnaissance studies into a period of problem-oriented scientific investigation. The International Geophysical Year and the intensive work of the 1960s and 1970s have established fundamental knowledge of Antarctic environmental systems on which present and future activities can be planned. Antarctic scientists of all nationalities are now eager to accept and exploit the challenges presented by global change programmes. At its XXth meeting in Hobart in September 1988, SCAR proposed an Antarctic component for inclusion in the ICSU International Geosphere–Biosphere Programme. Antarctic science thus considers itself sufficiently mature to be able to contribute effectively to programmes of world scope. Indeed, involvement in such activities may be seen as mandatory in order to continue to underscore the credibility and mainstream relevance of Antarctic scientific endeavours