Pharmacological modulation of diacylglycerol-sensitive TRPC3/6/7 channels

Current Pharmaceutical Biotechnology

Volumn 12, Issue 1, 2011, Pages 35-41

  Harteneck, Christian ^a   Gollasch, Maik ^b  

^a UNIVERSITY OF TÜBINGEN   (Germany)

^b CHARITÉ UNIVERSITÄTSMEDIZIN BERLIN   (Germany)

Author keywords

ACA; Calcium homeostasis; Diacylglycerol; Hyperforin; SFKF 96365

Indexed keywords

1 (5 CHLORO 1 NAPHTHALENESULFONYL)HEXAHYDRO 1H 1,4 DIAZEPINE; 1 [2 (4 METHOXYPHENYL) 2 [3 (4 METHOXYPHENYL)PROPOXY]ETHYL] 1H IMIDAZOLE; 2 AMINOETHOXYDIPHENYLBORANE; BARIUM ION; DIACYLGLYCEROL; GADOLINIUM; HYPERFORIN; INOSITOL 1,4,5 TRISPHOSPHATE RECEPTOR; LANTHANUM; MYOSIN LIGHT CHAIN KINASE; N (6 AMINOHEXYL) 1 NAPHTHALENESULFONAMIDE; N (6 AMINOHEXYL) 5 CHLORO 1 NAPHTHALENESULFONAMIDE; PYR 3; RECEPTOR BLOCKING AGENT; STRONTIUM; TRANSIENT RECEPTOR POTENTIAL CHANNEL 3; TRANSIENT RECEPTOR POTENTIAL CHANNEL 6; TRANSIENT RECEPTOR POTENTIAL CHANNEL 7; UNCLASSIFIED DRUG;

ARTICLE; CLINICAL TRIAL (TOPIC); HUMAN; META ANALYSIS (TOPIC); MODULATION; NONHUMAN; PROTEIN FUNCTION;

ANIMALS; CALCIUM; CALCIUM CHANNEL BLOCKERS; DIGLYCERIDES; HUMANS; MOLECULAR TARGETED THERAPY; PHOSPHOLIPASE C GAMMA; SIGNAL TRANSDUCTION; TRANSIENT RECEPTOR POTENTIAL CHANNELS; TRPC CATION CHANNELS;

EID: 78650857657     PISSN: 13892010     EISSN: 18734316     Source Type: Journal    
DOI: 10.2174/138920111793937943     Document Type: Article

References (67)

1. Hofmann, T.; Obukhov, A.G.; Schaefer, M.; Harteneck, C.; Gudermann, T.; Schultz, G. Direct activation of human TRPC6 andTRPC3 channels by diacylglycerol. Nature, 1999, 397(6716), 259-263.
2. Okada, T.; Inoue, R.; Yamazaki, K.; Maeda, A.; Kurosaki, T.; Yamakuni, T.; Tanaka, I.; Shimizu, S.; Ikenaka, K.; Imoto, K.; Mori, Y. Molecular and functional characterization of a novelmouse transient receptor potential protein homologue TRP7. Ca2+-permeable cation channel that is constitutively activated and enhancedby stimulation of G protein-coupled receptor. J. Biol.Chem., 1999, 274(39), 27359-27370.
3. Lucas, P.; Ukhanov, K.; Leinders-Zufall, T.; Zufall, F. A diacylglycerol-gated cation channel in vomeronasal neuron dendrites isimpaired in TRPC2 mutant mice: mechanism of pheromone transduction.Neuron, 2003, 40(3), 551-561.
4. Chyb, S.; Raghu, P.; Hardie, R.C. Polyunsaturated fatty acids activatethe Drosophila light-sensitive channels TRP and TRPL. Nature,1999, 397(6716), 255-259.
5. Jörs, S.; Kazanski, V.; Foik, A.; Krautwurst, D.; Harteneck, C.Receptor-induced activation of Drosophila TRP gamma by polyunsaturatedfatty acids. J. Biol. Chem., 2006, 281(40), 29693-29702.
6. Abramowitz, J. Birnbaumer, L. Physiology and pathophysiology ofcanonical transient receptor potential channels. FASEB J., 2009,23(2), 297-328.
7. Dietrich, A. Gudermann, T. Trpc6. Handb. Exp. Pharmacol., 2007,179, 125-141.
8. Eder, P.; Poteser, M.; Groschner, K. TRPC3: a multifunctional,pore-forming signalling molecule. Handb. Exp. Pharmacol., 2007,179, 77-92.
9. Numaga, T.; Wakamori, M.; Mori, Y. Trpc7. Handb. Exp. Pharmacol.,2007, 179, 143-151.
10. Inoue, R.; Okada, T.; Onoue, H.; Hara, Y.; Shimizu, S.; Naitoh, S.; Ito, Y.; Mori, Y. The transient receptor potential protein homologueTRP6 is the essential component of vascular alpha1-adrenoceptor-activated Ca2+-permeable cation channel. Circ. Res.,2001, 88(3), 325-332.
11. Vazquez, G.; Lievremont, J.P.; St, J.B.G.; Putney, J.W., Jr. HumanTrp3 forms both inositol trisphosphate receptor-dependent and receptor-independent store-operated cation channels in DT40 avian Blymphocytes. Proc. Natl. Acad. Sci. USA, 2001, 98(20), 11777-11782.
12. Boulay, G.; Zhu, X.; Peyton, M.; Jiang, M.; Hurst, R.; Stefani, E.; Birnbaumer, L. Cloning and expression of a novel mammalian homologof Drosophila transient receptor potential (Trp) involved incalcium entry secondary to activation of receptors coupled by theGq class of G protein. J. Biol. Chem., 1997, 272(47), 29672-29680.
13. Zhu, X.; Jiang, M.; Birnbaumer, L. Receptor-activated Ca2+ influxvia human Trp3 stably expressed in human embryonic kidney(HEK)293 cells. Evidence for a non-capacitative Ca2+ entry. J.Biol. Chem., 1998, 273(1), 133-142.
14. Halaszovich, C.R.; Zitt, C.; Jungling, E.; Lückhoff, A. Inhibition ofTRP3 channels by lanthanides. Block from the cytosolic side of theplasma membrane. J. Biol. Chem., 2000, 275(48), 37423-37428.
15. Riccio, A.; Mattei, C.; Kelsell, R.E.; Medhurst, A.D.; Calver, A.R.; Randall, A.D.; Davis, J.B.; Benham, C.D.; Pangalos, M.N. Cloningand functional expression of human short TRP7, a candidate proteinfor store-operated Ca2+ influx. J. Biol. Chem., 2002, 277(14),12302-12309.
16. Clementi, E.; Meldolesi, J. Pharmacological and functional propertiesof voltage-independent Ca2+ channels. Cell Calcium, 1996,19(4), 269-279.
17. Leung, Y.M.; Kwan, C.Y. Current perspectives in the pharmacologicalstudies of store-operated Ca2+ entry blockers. Jpn. J. Pharmacol.,1999, 81(3), 253-258.
18. Merritt, J.E.; Armstrong, W.P.; Benham, C.D.; Hallam, T.J.; Jacob, R.; JaxaChamiec, A.; Leigh, B.K.; McCarthy, S.A.; Moores, K.E.; Rink, T.J. SK&F 96365, a novel inhibitor of receptor-mediated calciumentry. Biochem. J., 1990, 271(2), 515-522.
19. Fasolato, C.; Pizzo, P.; Pozzan, T. Receptor-mediated calciuminflux in PC12 cells. ATP and bradykinin activate two independentpathways. J. Biol. Chem., 1990, 265(33), 20351-20355.
20. Krautwurst, D.; Hescheler, J.; Arndts, D.; Losel, W.; Hammer, R.; Schultz, G. Novel potent inhibitor of receptor-activated nonselectivecation currents in HL-60 cells. Mol. Pharmacol., 1993, 43(5),655-659.
21. Shlykov, S.G.; Yang, M.; Alcorn, J.L.; Sanborn, B.M. Capacitativecation entry in human myometrial cells and augmentation byhTrpC3 overexpression. Biol. Reprod., 2003, 69(2), 647-655.
22. Bootman, M.D.; Collins, T.J.; Mackenzie, L.; Roderick, H.L.; Berridge, M.J.; Peppiatt, C.M. 2-aminoethoxydiphenyl borate (2-APB) is a reliable blocker of store-operated Ca2+ entry but an inconsistentinhibitor of InsP3-induced Ca2+ release. FASEB J., 2002,16(10), 1145-1150.
23. van Rossum, D.B.; Patterson, R.L.; Ma, H.T.; Gill, D.L. Ca2+ entrymediated by store depletion, S-nitrosylation, and TRP3 channels.Comparison of coupling and function. J. Biol. Chem., 2000,275(37), 28562-28568.
24. Tesfai, Y.; Brereton, H.M.; Barritt, G.J. A diacylglycerol-activatedCa2+ channel in PC12 cells (an adrenal chromaffin cell line) correlateswith expression of the TRP-6 (transient receptor potential)protein. Biochem. J., 2001, 358(Pt 3), 717-726.
25. Hanano, T.; Hara, Y.; Shi, J.; Morita, H.; Umebayashi, C.; Mori, E.; Sumimoto, H.; Ito, Y.; Mori, Y.; Inoue, R. Involvement ofTRPM7 in cell growth as a spontaneously activated Ca2+ entrypathway in human retinoblastoma cells. J. Pharmacol. Sci., 2004,95(4), 403-419.
26. Xu, S.Z.; Zeng, F.; Boulay, G.; Grimm, C.; Harteneck, C.; Beech, D.J. Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: adifferential, extracellular and voltage-dependent effect. Br. J.Pharmacol., 2005, 145(4), 405-414.
27. Li, M.; Jiang, J.; Yue, L. Functional characterization of homo andheteromeric channel kinases TRPM6 and TRPM7. J. Gen. Physiol.,2006, 127(5), 525-537.
28. Voets, T.; Prenen, J.; Fleig, A.; Vennekens, R.; Watanabe, H.; Hoenderop, J.G.; Bindels, R.J.; Droogmans, G.; Penner, R.; Nilius, B. CaT1 and the calcium release-activated calcium channel manifestdistinct pore properties. J. Biol. Chem., 2001, 276(51), 47767-47770.
29. Chung, M.K.; Lee, H.; Mizuno, A.; Suzuki, M.; Caterina, M.J. 2-aminoethoxydiphenyl borate activates and sensitizes the heat-gatedion channel TRPV3. J. Neurosci., 2004, 24(22), 5177-5182.
30. Gu, Q.; Lin, R.L.; Hu, H.Z.; Zhu, M.X.; Lee, L.Y. 2-aminoethoxydiphenyl borate stimulates pulmonary C neurons viathe activation of TRPV channels. Am. J. Physiol. Lung Cell. Mol.Physiol., 2005, 288(5), L932-41.
31. Varnai, P.; Hunyady, L.; Balla, T. STIM and Orai: the long-awaitedconstituents of store-operated calcium entry. Trends Pharmacol.Sci., 2009, 30(3), 118-128.
32. Lis, A.; Peinelt, C.; Beck, A.; Parvez, S.; Monteilh-Zoller, M.; Fleig, A.; Penner, R. CRACM1, CRACM2, and CRACM3 arestore-operated Ca2+ channels with distinct functional properties.Curr. Biol., 2007, 17(9), 794-800.
33. Schindl, R.; Bergsmann, J.; Frischauf, I.; Derler, I.; Fahrner, M.; Muik, M.; Fritsch, R.; Groschner, K.; Romanin, C. 2-aminoethoxydiphenyl borate alters selectivity of Orai3 channels byincreasing their pore size. J. Biol. Chem., 2008, 283(29), 20261-20267.
34. Zhang, S.L.; Kozak, J.A.; Jiang, W.; Yeromin, A.V.; Chen, J.; Yu, Y.; Penna, A.; Shen, W.; Chi, V.; Cahalan, M.D. Store-dependentand -independent modes regulating Ca2+ release-activated Ca2+channel activity of human Orai1 and Orai3. J. Biol. Chem., 2008,283(25), 17662-17671.
35. Kraft, R.; Grimm, C.; Frenzel, H.; Harteneck, C. Inhibition ofTRPM2 cation channels by N-(p-amylcinnamoyl)anthranilic acid.Br. J. Pharmacol., 2006, 148(3), 264-273.
36. Harteneck, C.; Frenzel, H.; Kraft, R. N-(p-amylcinnamoyl) anthranilicacid (ACA): a phospholipase A2 inhibitor and TRP channelblocker. Cardiovasc. Drug Rev., 2007, 25(1), 61-75.
37. Shi, J.; Takahashi, S.; Jin, X.H.; Li, Y.Q.; Ito, Y.; Mori, Y.; Inoue, R. Myosin light chain kinase-independent inhibition by ML-9 ofmurine TRPC6 channels expressed in HEK293 cells. Br. J. Pharmacol.,2007, 152(1), 122-131.
38. Leuner, K.; Kazanski, V.; Müller, M.; Essin, K.; Henke, B.; Gollasch, M.; Harteneck, C.; Müller, W.E. Hyperforin-a key constituentof St. John's wort specifically activates TRPC6 channels.FASEB J., 2007, 21(14), 4101-4111.
39. Williams, J.W., Jr. Holsinger, T. St John's for depression, worts andall. BMJ, 2005, 330(7500), E350-351.
40. Lecrubier, Y.; Clerc, G.; Didi, R.; Kieser, M. Efficacy of St. John'swort extract WS 5570 in major depression: a double-blind, placebo-controlled trial. Am. J. Psychiatry, 2002, 159(8), 1361-1366.
41. Szegedi, A.; Kohnen, R.; Dienel, A.; Kieser, M. Acute treatment ofmoderate to severe depression with hypericum extract WS 5570 (StJohn's wort): randomised controlled double blind non-inferioritytrial versus paroxetine. BMJ, 2005, 330(7490), 503.
42. Kasper, S.; Gastpar, M.; Müller, W.E.; Volz, H.P.; Dienel, A.; Kieser, M.; Möller, H.J. Efficacy of St. John's wort extract WS5570 in acute treatment of mild depression: a reanalysis of datafrom controlled clinical trials. Eur. Arch. Psychiatry Clin. Neurosci.,2008, 258(1), 59-63.
43. Linde, K.; Berner, M.; Levente, K. St John's wort for major depression.Cochrane Database Syst. Rev., 2009, CD000448.
44. Singer, A.; Wonnemann, M.; Müller, W.E. Hyperforin, a majorantidepressant constituent of St. John's Wort, inhibits serotonin uptakeby elevating free intracellular Na+. J. Pharmacol. Exp. Ther.,1999, 290(3), 1363-1368.
45. Wonnemann, M.; Singer, A.; Müller, W.E. Inhibition of synaptosomaluptake of 3H-L-glutamate and 3H-GABA by hyperforin, amajor constituent of St. John's Wort: the role of amiloride sensitivesodium conductive pathways. Neuropsychopharmacology, 2000,23(2), 188-197.
46. Schempp, C.M.; Winghofer, B.; Ludtke, R.; Simon-Haarhaus, B.; Schopf, E.; Simon, J.C. Topical application of St John's wort (Hypericumperforatum L.) and of its metabolite hyperforin inhibits theallostimulatory capacity of epidermal cells. Br. J. Dermatol., 2000,142(5), 979-984.
47. Cai, S.; Fatherazi, S.; Presland, R.B.; Belton, C.M.; Izutsu, K.T. TRPC channel expression during calcium-induced differentiationof human gingival keratinocytes. J. Dermatol. Sci., 2005, 40(1), 21-28.
48. Beck, B.; Zholos, A.; Sydorenko, V.; Roudbaraki, M.; Lehen'kyi, V.; Bordat, P.; Prevarskaya, N.; Skryma, R. TRPC7 is a receptoroperatedDAG-activated channel in human keratinocytes. J. Invest.Dermatol., 2006, 126(9), 1982-1993.
49. Woelfle, U.; Laszczyk, M.N.; Kraus, M.; Leuner, K.; Kersten, A.; Simon-Haarhaus, B.; Scheffler, A.; Martin, S.F.; Müller, W.E.; Nashan, D.; Schempp, C.M. Triterpenes promote keratinocyte differentiationin vitro, ex vivo and in vivo: a role for the transient receptorpotential canonical (subtype) 6. J. Invest. Dermatol., 2010,130(1), 113-123.
50. Müller, M.; Essin, K.; Hill, K.; Beschmann, H.; Rubant, S.; Schempp, C.M.; Gollasch, M.; Boehncke, W.H.; Harteneck, C.; Müller, W.E.; Leuner, K. Specific TRPC6 channel activation, anovel approach to stimulate keratinocyte differentiation. J. Biol.Chem., 2008, 283(49), 33942-33954.
51. Chen, Y. Goldstein, J.A. The transcriptional regulation of the humanCYP2C genes. Curr. Drug Metab., 2009, 10(6), 567-578.
52. Whitten, D.L.; Myers, S.P.; Hawrelak, J.A.; Wohlmuth, H. Theeffect of St John's wort extracts on CYP3A: a systematic review ofprospective clinical trials. Br. J. Clin. Pharmacol., 2006, 62(5),512-526.
53. Hercule, H.C.; Schunck, W.H.; Gross, V.; Seringer, J.; Leung, F.P.; Weldon, S.M.; da Costa Goncalves, A.; Huang, Y.; Luft, F.C.; Gollasch, M. Interaction between P450 eicosanoids and nitric oxide inthe control of arterial tone in mice. Arterioscler. Thromb. Vasc.Biol., 2009, 29(1), 54-60.
54. Schroeder, C.; Tank, J.; Goldstein, D.S.; Stoeter, M.; Haertter, S.; Luft, F.C.; Jordan, J. Influence of St John's wort on catecholamineturnover and cardiovascular regulation in humans. Clin. Pharmacol.Ther., 2004, 76(5), 480-489.
55. Jung, S.; Strotmann, R.; Schultz, G.; Plant, T.D. TRPC6 is a candidatechannel involved in receptor-stimulated cation currents inA7r5 smooth muscle cells. Am. J. Physiol. Cell. Physiol., 2002,282(2), C347-59.
56. Dietrich, A.; Mederos, Y.S.M.; Gollasch, M.; Gross, V.; Storch, U.; Dubrovska, G.; Obst, M.; Yildirim, E.; Salanova, B.; Kalwa, H.; Essin, K.; Pinkenburg, O.; Luft, F.C.; Gudermann, T.; Birnbaumer, L. Increased vascular smooth muscle contractility in TRPC6-/-mice. Mol. Cell. Biol., 2005, 25(16), 6980-6989.
57. Brayden, J.E.; Earley, S.; Nelson, M.T.; Reading, S. Transientreceptor potential (TRP) channels, vascular tone and autoregulationof cerebral blood flow. Clin. Exp. Pharmacol. Physiol., 2008,35(9), 1116-1120.
58. Inoue, R.; Jian, Z.; Kawarabayashi, Y. Mechanosensitive TRPchannels in cardiovascular pathophysiology. Pharmacol. Ther.,2009, 123(3), 371-385.
59. Chatterjee, S.; Filippov, V.; Lishko, P.; Maximyuk, O.; Noldner, M.; Krishtal, O. Hyperforin attenuates various ionic conductancemechanisms in the isolated hippocampal neurons of rat. Life Sci.,1999, 65(22), 2395-2405.
60. Fisunov, A.; Lozovaya, N.; Tsintsadze, T.; Chatterjee, S.; Noldner, M.; Krishtal, O. Hyperforin modulates gating of P-type Ca2+ currentin cerebellar Purkinje neurons. Pflügers Arch., 2000, 440(3),427-434.
61. Winn, M.P.; Conlon, P.J.; Lynn, K.L.; Farrington, M.K.; Creazzo, T.; Hawkins, A.F.; Daskalakis, N.; Kwan, S.Y.; Ebersviller, S.; Burchette, J.L.; Pericak-Vance, M.A.; Howell, D.N.; Vance, J.M.; Rosenberg, P.B. A mutation in the TRPC6 cation channel causesfamilial focal segmental glomerulosclerosis. Science, 2005,308(5729), 1801-1804.
62. Reiser, J.; Polu, K.R.; Moller, C.C.; Kenlan, P.; Altintas, M.M.; Wei, C.; Faul, C.; Herbert, S.; Villegas, I.; Avila-Casado, C.; McGee, M.; Sugimoto, H.; Brown, D.; Kalluri, R.; Mundel, P.; Smith, P.L.; Clapham, D.E.; Pollak, M.R. TRPC6 is a glomerularslit diaphragm-associated channel required for normal renal function.Nat. Genet., 2005, 37(7), 739-744.
63. Kriz, W. TRPC6 a new podocyte gene involved in focal segmentalglomerulosclerosis. Trends Mol. Med., 2005, 11(12), 527-530.
64. Winn, M.P.; Daskalakis, N.; Spurney, R.F.; Middleton, J.P. Unexpectedrole of TRPC6 channel in familial nephrotic syndrome: doesit have clinical implications? J. Am. Soc. Nephrol., 2006, 17(2),378-387.
65. Leuner, K.; Heiser, J.H.; Derksen, S.; Mladenov, M.I.; Fehske, C.J.; Schubert, R.; Gollasch, M.; Schneider, G.; Harteneck, C.; Chatterjee, S.S.; Müller, W.E. Simple 2,4-diacylphloroglucinols asclassic transient receptor potential-6 activators-identification of anovel pharmacophore. Mol. Pharmacol., 2010, 77(3), 368-377.
66. Kiyonaka, S.; Kato, K.; Nishida, M.; Mio, K.; Numaga, T.; Sawaguchi, Y.; Yoshida, T.; Wakamori, M.; Mori, E.; Numata, T.; Ishii, M.; Takemoto, H.; Ojida, A.; Watanabe, K.; Uemura, A.; Kurose, H.; Morii, T.; Kobayashi, T.; Sato, Y.; Sato, C.; Hamachi, I.; Mori, Y. Selective and direct inhibition of TRPC3 channels underlies biologicalactivities of a pyrazole compound. Proc. Natl. Acad. Sci.USA, 2009, 106(13), 5400-5405.
67. Zitt, C.; Strauss, B.; Schwarz, E.C.; Spaeth, N.; Rast, G.; Hatzelmann, A.; Hoth, M. Potent inhibition of Ca2+ release-activated Ca2+channels and T-lymphocyte activation by the pyrazole derivativeBTP2. J. Biol. Chem., 2004, 279(13), 12427-12437.