2-aminoethoxydiphenyl borate activates the mechanically gated human KCNK channels KCNK 2 (TREK-1), KCNK 4 (TRAAK), and KCNK 10 (TREK-2)

Frontiers in Pharmacology

Volumn 4 MAY, Issue , 2013, Pages

  Beltrán, Leopoldo ^a   Beltrán, Madeline ^a   Aguado, Ainhara ^a   Gisselmann, Günter ^a   Hatt, Hanns ^a  

^a RUHR UNIVERSITY BOCHUM   (Germany)

Author keywords

2 APB; KCNK channels; TREK; Two electrode voltage clamp; Xenopus oocytes

Indexed keywords

2 AMINOETHOXYDIPHENYLBORANE; COMPLEMENTARY RNA; POTASSIUM CHANNEL; POTASSIUM CHANNEL KCNK 10; POTASSIUM CHANNEL KCNK 2; POTASSIUM CHANNEL KCNK 4; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CELL STRAIN HEK293; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFICACY; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; NONHUMAN; OOCYTE; VOLTAGE CLAMP TECHNIQUE; XENOPUS LAEVIS;

EID: 84881601510     PISSN: None     EISSN: 16639812     Source Type: Journal    
DOI: 10.3389/fphar.2013.00063     Document Type: Article

References (19)

1. Alloui, A., Zimmermann, K., Mamet, J., Duprat, F., Noël, J., Chemin, J., et al. (2006). TREK-1, a K+ channel involved in polymodal pain perception. EMBO J. 25, 2368-2376.
2. Bang, H., Kim, Y., and Kim, D. (2000). TREK-2, a new member of the mechanosensitive tandem-pore K+ channel family. J. Biol. Chem. 275, 17412-17419.
3. Dobrydneva, Y., and Blackmore, P. (2001). 2-Aminoethoxydiphenyl borate directly inhibits store-operated calcium entry channels in human platelets. Mol. Pharmacol. 3, 541-552.
4. Dörner, J. F., Gisselmann, G., Hatt, H., and Wetzel, C. H. (2007). Transient receptor potential channel A1 is directly gated by calcium ions. J. Biol. Chem. 282, 13180-13189.
5. Enyedi, P., and Czirják, G. (2010). Molecular background of leak K+ currents: two-pore domain potassium channels. Physiol. Rev. 90, 559-605.
6. Goldstein, S., Bockenhauer, D., O'Kelly, I., and Zilberberg, N. (2001). Potassium leak channels and the KCNK family of two-P-domain subunits. Nat. Rev. Neurosci. 2, 175-184.
7. Gu, W., Schlichthörl, G., Hirsch, J. R., Engels, H., Karschin, C., Karschin, A., et al. (2002). Expression pattern and functional characteristics of two novel splice variants of the two-pore-domain potassium channel TREK-2. J. Physiol. 539, 657-668.
8. Heurteaux, C., Lucas, G., Guy, N., El Yacoubi, M., Thümmler, S., Peng, X. D., et al. (2006). Deletion of the background potassium channel TREK-1 results in a depression-resistant phenotype. Nat. Neurosci. 9, 1134-1141.
9. Hu, H. Z., Gu, Q., Wang, C., Colton, C. K., Tang, J., Kinoshita-Kawada, M., et al. (2004). 2-Aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2, and TRPV3. J. Biol. Chem. 279, 35741-35748.
10. Kang, D., and Kim, D. (2006). TREK-2 (K2P10.1) and TRESK (K2P18.1) are major background K+ channels in dorsal root ganglion neurons. Am. J. Physiol. Cell Physiol. 291, C138-C146.
11. Kim, E. J., Kang, D., and Han, J. (2011). Baicalein and wogonin are activators of rat TREK-2 two-pore domain K+ channel. Acta Physiol. (Oxf.) 202, 185-192.
12. Lotshaw, D. P. (2007). Biophysical, pharmacological, and functional characteristics of cloned and native mammalian two-pore domain K+ channels. Cell Biochem. Biophys. 47, 209-256.
13. Maruyama, T., Kanaji, T., Nakade, S., Kanno, T., and Mikoshiba, K. (1997). 2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release. J. Biochem. 122, 498-505.
14. Medhurst, A. D., Rennie, G., Chapman, C. G., Meadows, H., Duckworth, M. D., Kelsell, R. E., et al. (2001). Distribution analysis of human two pore domain potassium channels in tissues of the central nervous system and periphery. Brain Res. Mol. Brain Res. 86, 101-114.
15. Noël, J., Zimmermann, K., Busserolles, J., Deval, E., Alloui, A., Diochot, S., et al. (2009). The mechano-activated K+ channels TRAAK and TREK-1 control both warm and cold perception. EMBO J. 28, 1308-1318.
16. Vogt-Eisele, A. K., Weber, K., Sherkheli, M. A., Vielhaber, G., Panten, J., Gisselmann, G., et al. (2007). Monoterpenoid agonists of TRPV3. Br. J. Pharmacol. 151, 530-540.
17. Wang, Y., Deshpande, M., and Payne, R. (2002). 2-Aminoethoxydiphenyl borate inhibits phototransduction and blocks voltage-gated potassium channels in Limulus ventral photoreceptors. Cell Calcium 4, 209-216.
18. Xian Tao, Li, Dyachenko, V., Zuzarte, M., Putzke, C., Preisig-Müller, R., Isenberg, G., et al. (2006). The stretch-activated potassium channel TREK-1 in rat cardiac ventricular muscle. Cardiovasc. Res. 69, 86-97.
19. Yamamoto, Y., Hatakeyama, T., and Taniguchi, K. (2009). Immunohistochemical colocalization of TREK-1, TREK-2 and TRAAK with TRP channels in the trigeminal ganglion cells. Neurosci. Lett. 454, 129-133.