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TRP channel activation by reversible covalent modification

Open access
Hinman, Andrew, Chuang, Huai-hu, Bautista, Diana M., Julius, David·2006·Proceedings of the National Academy of Sciences

Abstract

Allyl isothiocyanate, the pungent principle of wasabi and other mustard oils, produces pain by activating TRPA1, an excitatory ion channel on sensory nerve endings. Isothiocyanates are membrane-permeable electrophiles that form adducts with thiols and primary amines, suggesting that covalent modification, rather than classical lock-and-key binding, accounts for their agonist properties. Indeed, we show that thiol reactive compounds of diverse structure activate TRPA1 in a manner that relies on covalent modification of cysteine residues within the cytoplasmic N terminus of the channel. These findings suggest an unusual paradigm whereby natural products activate a receptor through direct, reversible, and covalent protein modification.

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Metadata

Authors
Hinman, A., Chuang, H.-H., Bautista, D. M., & Julius, D.
Venue
Proceedings of the National Academy of Sciences
Published
2006-12-19
Volume
103
Issue
51
Pages
19564-19568
ISSN
  • 0027-8424 (ISSN-L)
  • 1091-6490
OpenAlex
W2062978707
Cited by
890
References
1
FWCI
19.03
Type
journal article
Language
en
Open access
bronze

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CoChat. (2026). Citation check: TRP channel activation by reversible covalent modification. https://app.cochat.ai/papers/10.1073/pnas.0609598103
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Hinman, A., Chuang, H.-H., Bautista, D. M., & Julius, D. (2006). TRP channel activation by reversible covalent modification. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.0609598103

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

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