The DOI matches its Crossref record; 50 of the 50 references it cites were found in a registry or an index.
2-Aminoethoxydiphenyl Borate Is a Common Activator of TRPV1, TRPV2, and TRPV3
Open accessAbstract
The transient receptor potential (TRP) superfamily contains a large number of proteins encoding cation permeable channels that are further divided into TRPC (canonical), TRPM (melastatin), and TRPV (vanilloid) subfamilies. Among the six TRPV members, TRPV1, TRPV2, TRPV3, and TRPV4 form heat-activated cation channels, which serve diverse functions ranging from nociception to osmolality regulation. Although chemical activators for TRPV1 and TRPV4 are well documented, those for TRPV2 and TRPV3 are lacking. Here we show that in the absence of other stimuli, 2-aminoethoxydiphenyl borate (2APB) activates TRPV1, TRPV2, and TRPV3, but not TRPV4, TRPV5, and TRPV6 expressed in HEK293 cells. In contrast, 2APB inhibits the activity of TRPC6 and TRPM8 evoked by 1-oleolyl-2-acetyl-sn-glycerol and menthol, respectively. In addition, low levels of 2APB strongly potentiate the effect of capsaicin, protons, and heat on TRPV1 as well as that of heat on TRPV3 expressed in Xenopus oocytes. In dorsal root ganglia neurons, supra-additive stimulations were evoked by 2APB and capsaicin or 2APB and acid. Our data suggest the existence of a common activation mechanism for TRPV1, TRPV2, and TRPV3 that may serve as a therapeutic target for pain management and treatment for diseases caused by hypersensitivity and temperature misregulation.
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Cited by
Store-Operated Calcium Channels
Parekh, A. B., & Putney, J. W. (2005) · Physiological Reviews · doi:10.1152/physrev.00057.2003 · Cited by 2,089
The thermo‐TRP ion channel family: properties and therapeutic implications
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Juszczak, G. R., & Swiergiel, A. H. (2009) · Progress in Neuro-Psychopharmacology and Biological Psychiatry · doi:10.1016/j.pnpbp.2008.12.014 · Cited by 211
TRPV3 regulates nitric oxide synthase-independent nitric oxide synthesis in the skin
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Metadata
- Authors
- Hu, H.-Z., Gu, Q., Wang, C., Colton, C. K., Tang, J., Kinoshita-Kawada, M., Lee, L.-Y., Wood, J. D., & Zhu, M. X.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 2004-08
- Volume
- 279
- Issue
- 34
- Pages
- 35741-35748
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W1970629236
- Cited by
- 517
- References
- 50
- FWCI
- 13.04
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Hu, H.-Z., Gu, Q., Wang, C., Colton, C. K., Tang, J., Kinoshita-Kawada, M., Lee, L.-Y., Wood, J. D., & Zhu, M. X. (2004). 2-Aminoethoxydiphenyl Borate Is a Common Activator of TRPV1, TRPV2, and TRPV3. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.m404164200
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