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Showing 1–3 of 3 results
Advanced filters: Author: Meriem Semache Clear advanced filters

  • Tummino et al. dock 74 million molecules against the human cannabinoid-1 receptor to find uM ligands. Optimization led to a nM agonist conferring analgesia with reduced side effects in mice, highlighting its potential as a pain therapeutic and the promise of a structure-based approach.

    • Tia A. Tummino
    • Christos Iliopoulos-Tsoutsouvas
    • Brian K. Shoichet
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-19

  • UCN2 acts as a ligand for the GPCR CRHR2 and there have been conflicting reports on whether UCN2 treatment improves or worsens glucose tolerance. Here, the authors show that acute UCN2 recruits Gs and decreases glucose uptake, while chronic treatment desensitizes CRHR2 and improves glucose uptake.

    • Stephen E. Flaherty III
    • Olivier Bezy
    • Zhidan Wu
    ResearchOpen Access
    Nature Communications
    Volume: 14, P: 1-16

  • Avet et al. characterize I-287, an inhibitor to protease-activated receptor 2 using BRET-assays. They find that I-287 selectively inhibits Gαq and Gα12/13 without affecting the activation of Gi/o or the recruitment of βarrestin2 and that it blocks inflammation in vitro and in vivo.

    • Charlotte Avet
    • Claudio Sturino
    • Michel Bouvier
    ResearchOpen Access
    Communications Biology
    Volume: 3, P: 1-13