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TRPV1 shows dynamic ionic selectivity during agonist stimulation.
Nat Neurosci. 2008 May; 11(5):555-64.NN

Abstract

Transient receptor potential vanilloid 1 (TRPV1) is an ion channel that is gated by noxious heat, capsaicin and other diverse stimuli. It is a nonselective cation channel that prefers Ca2+ over Na+. These permeability characteristics, as in most channels, are widely presumed to be static. On the contrary, we found that activation of native or recombinant rat TRPV1 leads to time- and agonist concentration-dependent increases in relative permeability to large cations and changes in Ca2+ permeability. Using the substituted cysteine accessibility method, we saw that these changes were attributable to alterations in the TRPV1 selectivity filter. TRPV1 agonists showed different capabilities for evoking ionic selectivity changes. Furthermore, protein kinase C-dependent phosphorylation of Ser800 in the TRPV1 C terminus potentiated agonist-evoked ionic selectivity changes. Thus, the qualitative signaling properties of TRPV1 are dynamically modulated during channel activation, a process that probably shapes TRPV1 participation in pain, cytotoxicity and neurotransmitter release.

Authors+Show Affiliations

Department of Biological Chemistry, Center for Sensory Biology, Johns Hopkins School of Medicine, 725 North Wolfe Street, Baltimore, Maryland 21205, USA.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

18391945

Citation

Chung, Man-Kyo, et al. "TRPV1 Shows Dynamic Ionic Selectivity During Agonist Stimulation." Nature Neuroscience, vol. 11, no. 5, 2008, pp. 555-64.
Chung MK, Güler AD, Caterina MJ. TRPV1 shows dynamic ionic selectivity during agonist stimulation. Nat Neurosci. 2008;11(5):555-64.
Chung, M. K., Güler, A. D., & Caterina, M. J. (2008). TRPV1 shows dynamic ionic selectivity during agonist stimulation. Nature Neuroscience, 11(5), 555-64. https://doi.org/10.1038/nn.2102
Chung MK, Güler AD, Caterina MJ. TRPV1 Shows Dynamic Ionic Selectivity During Agonist Stimulation. Nat Neurosci. 2008;11(5):555-64. PubMed PMID: 18391945.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - TRPV1 shows dynamic ionic selectivity during agonist stimulation. AU - Chung,Man-Kyo, AU - Güler,Ali D, AU - Caterina,Michael J, Y1 - 2008/04/06/ PY - 2008/01/25/received PY - 2008/02/19/accepted PY - 2008/4/9/pubmed PY - 2008/7/1/medline PY - 2008/4/9/entrez SP - 555 EP - 64 JF - Nature neuroscience JO - Nat Neurosci VL - 11 IS - 5 N2 - Transient receptor potential vanilloid 1 (TRPV1) is an ion channel that is gated by noxious heat, capsaicin and other diverse stimuli. It is a nonselective cation channel that prefers Ca2+ over Na+. These permeability characteristics, as in most channels, are widely presumed to be static. On the contrary, we found that activation of native or recombinant rat TRPV1 leads to time- and agonist concentration-dependent increases in relative permeability to large cations and changes in Ca2+ permeability. Using the substituted cysteine accessibility method, we saw that these changes were attributable to alterations in the TRPV1 selectivity filter. TRPV1 agonists showed different capabilities for evoking ionic selectivity changes. Furthermore, protein kinase C-dependent phosphorylation of Ser800 in the TRPV1 C terminus potentiated agonist-evoked ionic selectivity changes. Thus, the qualitative signaling properties of TRPV1 are dynamically modulated during channel activation, a process that probably shapes TRPV1 participation in pain, cytotoxicity and neurotransmitter release. SN - 1097-6256 UR - https://www.unboundmedicine.com/medline/citation/18391945/TRPV1_shows_dynamic_ionic_selectivity_during_agonist_stimulation_ L2 - https://doi.org/10.1038/nn.2102 DB - PRIME DP - Unbound Medicine ER -