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An Extracellular Pore‑Targeting Peptide Defines a Designable Allosteric Site in TRPV2

open access: yesAdvanced Science, EarlyView.
Structure‐guided peptide engineering yields Depiv2, a highly potent and subtype‐selective TRPV2 inhibitor that binds to the extracellular pore and remodels it into a closed, non‐conductive state. Depiv2 suppresses pathological cardiac hypertrophy, establishing the TRPV2 outer pore as a designable interface for selective peptide modulation.
Aiqin Zhu   +7 more
wiley   +1 more source
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