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Showing 1–6 of 6 results
Advanced filters: Author: Peter Scammells Clear advanced filters
  • MIPS521, a positive allosteric modulator of the adenosine A1 receptor, has analgesic properties in a rat model of neuropathic pain through a mechanism by which MIPS521 stabilizes the complex between adenosine, receptor and G protein.

    • Christopher J. Draper-Joyce
    • Rebecca Bhola
    • Arthur Christopoulos
    Research
    Nature
    Volume: 597, P: 571-576
  • Allosteric GPCR modulators can achieve exquisite subtype selectivity, but the underlying mechanism is unclear. Using molecular dynamics simulations, the authors here identify a previously undetected dynamic pocket in muscarinic GPCRs that is critical for subtype selectivity of allosteric modulators.

    • Scott A. Hollingsworth
    • Brendan Kelly
    • Ron O. Dror
    ResearchOpen Access
    Nature Communications
    Volume: 10, P: 1-9
  • Biased agonists act at a receptor to preferentially induce distinct intracellular signalling responses over others. Here the authors show how kinetics of ligand binding and signaling responses greatly influence observed bias profiles, and hence must be considered when studying biased agonists.

    • Carmen Klein Herenbrink
    • David A. Sykes
    • J. Robert Lane
    ResearchOpen Access
    Nature Communications
    Volume: 7, P: 1-14
  • A compound previously identified as a dopamine D2 receptor allosteric modulator was found to be a bitopic ligand that binds the orthosteric and allosteric sites to allow binding to one D2 protomer and allosteric modulation of the associated protomer.

    • J Robert Lane
    • Prashant Donthamsetti
    • Arthur Christopoulos
    Research
    Nature Chemical Biology
    Volume: 10, P: 745-752
  • Very little is known about how a G-protein-coupled receptor (GPCR) transitions from an inactive to an active state, but this study has solved the X-ray crystal structures of the human M2 muscarinic acetylcholine receptor bound to a high-affinity agonist in an active state and to a high-affinity agonist and a small-molecule allosteric modulator in an active state; the structures provide insights into the activation mechanism and allosteric modulation of muscarinic receptors.

    • Andrew C. Kruse
    • Aaron M. Ring
    • Brian K. Kobilka
    Research
    Nature
    Volume: 504, P: 101-106