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• W4377010868 abstract "The cation-permeable TRPV2 channel is important for cardiac and immune cell function. Cannabidiol (CBD), a non-psychoactive cannabinoid of clinical relevance, is one of the few molecules known to activate TRPV2. Using the patch-clamp technique, we discover that CBD can sensitize current responses of the rat TRPV2 channel to the synthetic agonist 2-aminoethoxydiphenyl borate (2-APB) by over two orders of magnitude, without sensitizing channels to activation by moderate (40°C) heat. Using cryo-EM, we uncover a new small-molecule binding site in the pore domain of rTRPV2 in addition to a nearby CBD site that had already been reported. The TRPV1 and TRPV3 channels are also activated by 2-APB and CBD and share multiple conserved features with TRPV2, but we find that strong sensitization by CBD is only observed in TRPV3, while sensitization for TRPV1 is much weaker. Mutations at non-conserved positions between rTRPV2 and rTRPV1 in either the pore domain or the CBD sites failed to confer strong sensitization by CBD in mutant rTRPV1 channels. Together, our results indicate that CBD-dependent sensitization of rTRPV2 channels engages multiple channel regions, and that the difference in sensitization strength between rTRPV2 and rTRPV1 channels does not originate from amino acid sequence differences at the CBD binding site or the pore domain. The remarkably robust effect of CBD on TRPV2 and TRPV3 channels offers a promising new tool to both understand and overcome one of the major roadblocks in the study of these channels - their resilience to activation." @default.
• W4377010868 created "2023-05-19" @default.
• W4377010868 creator A5008919071 @default.
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• W4377010868 date "2023-05-18" @default.
• W4377010868 modified "2023-10-17" @default.
• W4377010868 title "Cannabidiol sensitizes TRPV2 channels to activation by 2-APB" @default.
• W4377010868 cites W1488329806 @default.
• W4377010868 cites W1495409864 @default.
• W4377010868 cites W1511198581 @default.
• W4377010868 cites W1534752717 @default.
• W4377010868 cites W1806267750 @default.
• W4377010868 cites W1840415699 @default.
• W4377010868 cites W1964159573 @default.
• W4377010868 cites W1965985711 @default.
• W4377010868 cites W1970629236 @default.
• W4377010868 cites W1988407098 @default.
• W4377010868 cites W1991972386 @default.
• W4377010868 cites W1995374814 @default.
• W4377010868 cites W2001734687 @default.
• W4377010868 cites W2003403297 @default.
• W4377010868 cites W2006849038 @default.
• W4377010868 cites W2011295158 @default.
• W4377010868 cites W2030623240 @default.
• W4377010868 cites W2033979022 @default.
• W4377010868 cites W2039263844 @default.
• W4377010868 cites W2042968117 @default.
• W4377010868 cites W2059398421 @default.
• W4377010868 cites W2061108756 @default.
• W4377010868 cites W2067436635 @default.
• W4377010868 cites W2071752189 @default.
• W4377010868 cites W2087381327 @default.
• W4377010868 cites W2088764206 @default.
• W4377010868 cites W2091994158 @default.
• W4377010868 cites W2100241249 @default.
• W4377010868 cites W2103826070 @default.
• W4377010868 cites W2105515899 @default.
• W4377010868 cites W2117226055 @default.
• W4377010868 cites W2124026197 @default.
• W4377010868 cites W2132629607 @default.
• W4377010868 cites W2135609872 @default.
• W4377010868 cites W2138841389 @default.
• W4377010868 cites W2142161929 @default.
• W4377010868 cites W2153704362 @default.
• W4377010868 cites W2161900438 @default.
• W4377010868 cites W2166903664 @default.
• W4377010868 cites W2171717653 @default.
• W4377010868 cites W2179650332 @default.
• W4377010868 cites W2180229411 @default.
• W4377010868 cites W2273228306 @default.
• W4377010868 cites W2279923977 @default.
• W4377010868 cites W2301186499 @default.
• W4377010868 cites W2323300135 @default.
• W4377010868 cites W2340643499 @default.
• W4377010868 cites W2394294586 @default.
• W4377010868 cites W2404622021 @default.
• W4377010868 cites W2421422434 @default.
• W4377010868 cites W2593511418 @default.
• W4377010868 cites W2790248681 @default.
• W4377010868 cites W2799315094 @default.
• W4377010868 cites W2809477862 @default.
• W4377010868 cites W2885180300 @default.
• W4377010868 cites W2887583364 @default.
• W4377010868 cites W2895963202 @default.
• W4377010868 cites W2900080727 @default.
• W4377010868 cites W2900599829 @default.
• W4377010868 cites W2903222042 @default.
• W4377010868 cites W2943925785 @default.
• W4377010868 cites W2949402747 @default.
• W4377010868 cites W2953320394 @default.
• W4377010868 cites W2966310203 @default.
• W4377010868 cites W2978944334 @default.
• W4377010868 cites W2983603509 @default.
• W4377010868 cites W2984139755 @default.
• W4377010868 cites W2986511781 @default.
• W4377010868 cites W2987639883 @default.
• W4377010868 cites W3008374358 @default.
• W4377010868 cites W3035806878 @default.
• W4377010868 cites W3036117037 @default.
• W4377010868 cites W3111745362 @default.
• W4377010868 cites W3130321125 @default.
• W4377010868 cites W3172268669 @default.
• W4377010868 cites W3196985151 @default.
• W4377010868 cites W4220824989 @default.
• W4377010868 cites W4225149868 @default.
• W4377010868 cites W4247052853 @default.
• W4377010868 cites W4252314477 @default.
• W4377010868 cites W4297241791 @default.
• W4377010868 cites W4310959645 @default.
• W4377010868 doi "https://doi.org/10.7554/elife.86166" @default.
• W4377010868 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/37199723" @default.
• W4377010868 hasPublicationYear "2023" @default.
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