Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2011 Nov 20;8(1):78-85.
doi: 10.1038/nchembio.712.

Lysophosphatidic acid directly activates TRPV1 through a C-terminal binding site

Andrés Nieto-Posadas  1 , Giovanni Picazo-Juárez, Itzel Llorente, Andrés Jara-Oseguera, Sara Morales-Lázaro, Diana Escalante-Alcalde, León D Islas, Tamara Rosenbaum
Affiliations

Lysophosphatidic acid directly activates TRPV1 through a C-terminal binding site

Andrés Nieto-Posadas et al. Nat Chem Biol. .

Erratum in

  • Nat Chem Biol. 2012 Aug;8(8):737. Dosage error in article text

Abstract

Since 1992, there has been growing evidence that the bioactive phospholipid lysophosphatidic acid (LPA), whose amounts are increased upon tissue injury, activates primary nociceptors resulting in neuropathic pain. The TRPV1 ion channel is expressed in primary afferent nociceptors and is activated by physical and chemical stimuli. Here we show that in control mice LPA produces acute pain-like behaviors, which are substantially reduced in Trpv1-null animals. Our data also demonstrate that LPA activates TRPV1 through a unique mechanism that is independent of G protein-coupled receptors, contrary to what has been widely shown for other ion channels, by directly interacting with the C terminus of the channel. We conclude that TRPV1 is a direct molecular target of the pain-producing molecule LPA and that this constitutes, to our knowledge, the first example of LPA binding directly to an ion channel to acutely regulate its function.

PubMed Disclaimer

Comment in

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. Neuroscience. 2008 Mar 18;152(2):296-8 - PubMed
    1. Proc Natl Acad Sci U S A. 2007 Jun 12;104(24):10246-51 - PubMed
    1. J Neurochem. 2010 Nov;115(3):643-53 - PubMed
    1. Prostaglandins Other Lipid Mediat. 2010 Apr;91(3-4):130-8 - PubMed
    1. Curr Mol Pharmacol. 2008 Nov;1(3):255-69 - PubMed

Publication types

LinkOut - more resources