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Structural mechanisms of TRPV2 modulation by endogenous and exogenous ligands - Nature Chemical Biology

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Structural mechanisms of TRPV2 modulation by endogenous and exogenous ligands - Nature Chemical Biology

The transient receptor potential vanilloid 2 (TRPV2) ion channel is a polymodal receptor widely involved in many physiological and pathological processes. Despite many TRPV2 modulators being identified, whether and how TRPV2 is regulated by endogenous lipids remains elusive. Here, we report an endogenous cholesterol molecule inside the vanilloid binding pocket (VBP) of TRPV2, with a 'head down, tail up' configuration, resolved at 3.2 Å using cryo-EM.

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Structural mechanisms of TRPV2 modulation by endogenous and exogenous ligands - Nature Chemical Biology

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Structural mechanisms of TRPV2 modulation by endogenous and exogenous ligands - Nature Chemical Biology

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