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Showing 1–5 of 5 results
Advanced filters: Author: "Nathanael S Gray" Clear advanced filters

  • High-throughput profiling of compound libraries against large panels of kinases is becoming technically feasible. In contrast to the traditional linear, target-centric approach to discovery, this approach may provide a choice of targets to pursue that is guided by the quality of lead compounds available, rather than by target biology alone, and could thereby significantly improve the productivity of kinase inhibitor discovery.

    • David M. Goldstein
    • Nathanael S. Gray
    • Patrick P. Zarrinkar
    Reviews
    Nature Reviews Drug Discovery
    Volume: 7, P: 391-397

  • Protein kinases have emerged as one of the most successful families of drug targets. To date, most selective kinase inhibitors have been discovered serendipitously either through broad selectivity screening or through the discovery of unique binding modes. Here we discuss design strategies that could lead to a broader coverage of the kinome with selective inhibitors and to a more rational approach for developing them.

    • Susanne Müller
    • Apirat Chaikuad
    • Stefan Knapp
    Comments & Opinion
    Nature Chemical Biology
    Volume: 11, P: 818-821

  • Inhibition of kinase activity has received enormous interest as a therapeutic strategy for cancer. This Review discusses the current approaches to develop and characterize new inhibitors.

    • Jianming Zhang
    • Priscilla L. Yang
    • Nathanael S. Gray
    Reviews
    Nature Reviews Cancer
    Volume: 9, P: 28-39

  • Chemical probes are urgently needed to functionally annotate hitherto-untargeted kinases and stimulate new drug discovery efforts to address unmet medical needs. The size of the human kinome combined with the high cost associated with probe generation severely limits access to new probes. We propose a large-scale public-private partnership as a new approach that offers economies of scale, minimized redundancy and sharing of risk and cost.

    • Stefan Knapp
    • Paulo Arruda
    • William J Zuercher
    Comments & Opinion
    Nature Chemical Biology
    Volume: 9, P: 3-6

  • The dysregulated activity of protein kinases is commonly implicated in human cancers, and many anti-cancer agents aiming to inhibit specific kinases are now approved or under investigation. Here, Settleman and colleagues discuss factors responsible for the variability in clinical sensitivity to small-molecule kinase inhibitors that should be considered in the development and use of new agents.

    • Pasi A. Jänne
    • Nathanael Gray
    • Jeff Settleman
    Reviews
    Nature Reviews Drug Discovery
    Volume: 8, P: 709-723