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Showing 1–7 of 7 results
Advanced filters: Author: Kaavya Krishna Kumar Clear advanced filters

  • This manuscript describes the structure of an endocannabinoid analog-bound CB1 complex and reveals the structural determinants of ligand efficacy. The activation mechanism, unique to CB1, that is exploited by allosteric modulators is also outlined.

    • Kaavya Krishna Kumar
    • Michael J. Robertson
    • Brian Kobilka
    ResearchOpen Access
    Nature Communications
    Volume: 14, P: 1-11

  • We propose a model for a sequential, multistep activation mechanism of metabotropic glutamate receptor subtype 5, including a series of structures in lipid nanodiscs, from inactive to fully active, with agonist-bound intermediate states.

    • Kaavya Krishna Kumar
    • Haoqing Wang
    • Brian K. Kobilka
    Research
    Nature
    Volume: 629, P: 951-956

  • A peripherally restricted CB1 agonist (VIP36) targeting a cryptic receptor pocket was developed, showing high efficacy in mouse pain models with minimal side effects and tolerance, potentially revolutionizing chronic pain treatment and GPCR drug design.

    • Vipin Ashok Rangari
    • Evan S. O’Brien
    • Susruta Majumdar
    Research
    Nature
    Volume: 640, P: 265-273

  • 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

  • A newly discovered negative allosteric modulator of the µ-opioid receptor works together with naloxone to potently block opioid agonist signalling with reduced adverse effects.

    • Evan S. O’Brien
    • Vipin Ashok Rangari
    • Brian K. Kobilka
    Research
    Nature
    Volume: 631, P: 686-693

  • Cryo-electron microscopy structures of human neurotensin receptor 1 in complex with Gi1 protein and the agonist JMV449 reveal a non-canonical state that may represent an intermediate form in G-protein activation.

    • Hideaki E. Kato
    • Yan Zhang
    • Georgios Skiniotis
    Research
    Nature
    Volume: 572, P: 80-85