2022
DOI: 10.22541/au.166299307.78275508/v1
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A rationally designed peptidomimetic modulator of CaV2.2 (N-type) voltage-gated calcium channels for chronic pain

Abstract: Background and Purpose Transmembrane Cav2.2 (N-type) voltage-gated calcium channels are genetically and pharmacologically validated pain targets. Clinical block of Cav2.2 (e.g., with Prialt) or indirect modulation (e.g., with gabapentinoids) mitigates chronic pain but is constrained by side effects. The cytosolic auxiliary subunit collapsin response mediator protein 2 (CRMP2) targets Cav2.2 to the sensory neuron membrane and regulates their function. A CRMP2-derived peptide (CBD3) uncouples the Cav2.2-CRMP2 in… Show more

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