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Showing 1–5 of 5 results
Advanced filters: Author: Prabha Ibrahim Clear advanced filters

  • PLX4032 is a selective inhibitor of the B-RAF protein that has shown promising results in an early clinical trial in melanoma patients with an activating mutation in B-RAF. Now the structure and function of this inhibitor are described. Translational data from a phase I trial show that clinical efficacy requires a substantial degree of inhibition of the ERK pathway downstream of B-RAF. The data also show that BRAF-mutant melanomas are highly dependent on B-RAF activity.

    • Gideon Bollag
    • Peter Hirth
    • Keith Nolop
    Research
    Nature
    Volume: 467, P: 596-599

  • Genetics implicate microglia in Alzheimer’s disease pathogenesis, but their roles remain unclear. Here, the authors find that microglial depletion in a mouse model of Alzheimer’s disease impairs plaque formation and that Aβ-induced changes in neuronal gene expression are microglia-mediated.

    • Elizabeth Spangenberg
    • Paul L. Severson
    • Kim N. Green
    ResearchOpen Access
    Nature Communications
    Volume: 10, P: 1-21

  • Vemurafenib is a small-molecule inhibitor of the oncogenic BRAF kinase approved for the treatment of melanoma. Here, the scientists involved in the discovery of vemurafenib describe the underlying biology of BRAF, the technology used to identify vemurafenib and its clinical development milestones, along with future prospects based on lessons learned during its development.

    • Gideon Bollag
    • James Tsai
    • Peter Hirth
    Reviews
    Nature Reviews Drug Discovery
    Volume: 11, P: 873-886

  • Next-generation RAF inhibitors that inhibit oncogenic BRAF without inducing paradoxical pathway activation in cells with mutant RAS might yield improved safety and more durable efficacy.

    • Chao Zhang
    • Wayne Spevak
    • Gideon Bollag
    Research
    Nature
    Volume: 526, P: 583-586