The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
A Bivalent Tarantula Toxin Activates the Capsaicin Receptor, TRPV1, by Targeting the Outer Pore Domain
Open accessAbstract
SUMMARY Toxins have evolved to target regions of membrane ion channels that underlie ligand binding, gating, or ion permeation, and have thus served as invaluable tools for probing channel structure and function. Here we describe a peptide toxin from the Earth Tiger tarantula that selectively and irreversibly activates the capsaicin- and heat-sensitive channel, TRPV1. This high avidity interaction derives from a unique tandem repeat structure of the toxin that endows it with an antibody-like bivalency, illustrating a new paradigm in toxin structure and evolution. The ‘double-knot’ toxin traps TRPV1 in the open state by interacting with residues in the presumptive pore-forming region of the channel, highlighting the importance of conformational changes in the outer pore region of TRP channels during activation.
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Citations
Cites
Molecular mechanisms of nociception
Julius, D., & Basbaum, A. I. (2001) · Nature · doi:10.1038/35093019 · Cited by 2,685 · cited 1×
“Chief among these is TRPV1, which is activated by capsaicin (the main pungent ingredient in ‘‘hot’’ chili peppers), extracellular protons, and other inflammation agents, as well as noxious heat (>43 C) (Julius and Basbaum, 2001).”
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Cited by
Chemosensory properties of the trigeminal system
Viana, F. (2011) · ACS Chemical Neuroscience · doi:10.1021/cn100102c · Cited by 196
Garami, A., Shimansky, Y. P., Rumbus, Z., Vizin, R. C. L., Farkas, N., Hegyi, J., Szakacs, Z., Solymar, M., Csenkey, A., Chiche, D. A., et al. (2020) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2020.107474 · Cited by 159
Pickering, G., Creveaux, I., Macian, N., & Pereira, B. (2020) · Pain Medicine · doi:10.1093/pm/pnz037 · Cited by 23
Zinc activation of OTOP proton channels identifies structural elements of the gating apparatus
Teng, B., Kaplan, J. P., Liang, Z., Chyung, K. S., Goldschen-Ohm, M. P., & Liman, E. R. (2023) · eLife · doi:10.7554/elife.85317 · Cited by 16
Metadata
- Authors
- Bohlen, C. J., Priel, A., Zhou, S., King, D., Siemens, J., & Julius, D.
- Venue
- Cell
- Publisher
- Elsevier BV
- Published
- 2010-05
- Volume
- 141
- Issue
- 5
- Pages
- 834-845
- ISSN
- 0092-8674 (ISSN-L)
- OpenAlex
- W2039263844
- Cited by
- 311
- References
- 1
- FWCI
- 9.76
- Type
- journal article
- Language
- en
- Open access
- bronze
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