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Showing 1–2 of 2 results
Advanced filters: Author: Daniel V. Sietsema Clear advanced filters

  • Cyclic GMP-AMP synthase (cGAS), an intracellular sensor of dsDNA, is a central driver of inflammatory diseases and an emerging therapeutic target, although optimization of cGAS inhibitors for the clinic is challenging because of the incomplete understanding of their mode of action. Here, the authors study the binding mode of G-chemotype human cGAS inhibitors, revealing key structural differences driving cGAS inhibitor cross-species potency shifts, and discover a novel cGAS inhibitor with exceptional mouse and human potency.

    • Alexander M. Skeldon
    • Li Wang
    • Kelly A. Pike
    ResearchOpen Access
    Communications Chemistry
    Volume: 8, P: 1-15

  • Polarisation of epithelial cells causes lumen formation, which is mediated by apical membrane initiation site (AMIS) and FIP5, but how this is regulated is unclear. Here, the authors identify cingulin as a FIP-5 interacting protein, recruiting the Rac1-WAVE/Scar complex to the AMIS and branched actin formation.

    • Anthony J. Mangan
    • Daniel V. Sietsema
    • Rytis Prekeris
    ResearchOpen Access
    Nature Communications
    Volume: 7, P: 1-15