4.7 Article

TRPV1 Activation by Anandamide via a Unique Lipid Pathway

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JOURNAL OF CHEMICAL INFORMATION AND MODELING
卷 61, 期 12, 页码 5742-5746

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AMER CHEMICAL SOC
DOI: 10.1021/acs.jcim.1c00893

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  1. National Institute on Drug Abuse [R01 DA003934]
  2. Pittsburgh Supercomputing Center (PSC) [R01GM116961, MCB190081P]

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This study reveals that the endocannabinoid anandamide can activate the TRPV1 channel at a unique peripheral binding site, expanding the knowledge of TRPV1 and aiding in the development of new TRPV1 modulators.
The capsaicin receptor, transient receptor potential vanilloid type 1 (TRPV1), is a polymodal channel that has been implicated in the perception of pain and can be modulated by a variety of cannabinoid ligands. Here we report TRPV1 channel activation by the endocannabinoid, anandamide (AEA), in a unique, peripheral binding site via extended MD simulations. These results aim to expand the understanding of TRPV1 and assist in the development of new TRPV1 modulators.

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