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Showing 1–5 of 5 results
Advanced filters: Author: Christopher J Draper-Joyce Clear advanced filters

  • The cryo-electron microscopy structure of the human adenosine A1 receptor in complex with adenosine and heterotrimeric Gi2 protein provides molecular insights into receptor and G-protein selectivity.

    • Christopher J. Draper-Joyce
    • Maryam Khoshouei
    • Arthur Christopoulos
    Research
    Nature
    Volume: 558, P: 559-563

  • 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

  • Activation signals from GPCRs, the largest receptor family, are transmitted to heterotrimeric G proteins and arrestins, and can be differentially modulated by GPCR phosphorylation. In a recent article, available data, including multiple arrestin structures, are analyzed to decipher common and state-specific conformational changes in arrestins and how these depend on patterns of receptor phosphorylation.

    • Christopher J. Draper-Joyce
    • Arthur Christopoulos
    News & Views
    Nature Structural & Molecular Biology
    Volume: 25, P: 437-439

  • 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