Fenamates as TRP channel blockers: Mefenamic acid selectively blocks TRPM3

British Journal of Pharmacology

Volumn 162, Issue 8, 2011, Pages 1757-1769

  Klose, Chihab ^a,b,c   Straub, Isabelle ^b,d   Riehle, Marc ^a   Ranta, Felicia ^a   Krautwurst, Dietmar ^e   Ullrich, Susanne ^a   Meyerhof, Wolfgang ^f   Harteneck, Christian ^a,b  

^a UNIVERSITY OF TÜBINGEN   (Germany)

^b CHARITÉ UNIVERSITÄTSMEDIZIN BERLIN   (Germany)

^c FREIE UNIVERSITÄT BERLIN   (Germany)

^d Rudolf Boehm Institut für Pharmakologie und Toxikologie   (Germany)

^e DEUTSCHE FORSCHUNGSANSTALT FÜR LEBENSMITTELCHEMIE   (Germany)

^f GERMAN INSTITUTE OF HUMAN NUTRITION   (Germany)

Author keywords

cationic channel; fenamate; non steroidal anti inflammatory drugs; pancreatic cells; transient receptor potential

Indexed keywords

3' 5 DICHLORODIPHENYLAMINE 2 CARBOXYLIC ACID; CALCIUM ION; FENAMIC ACID DERIVATIVE; FLUFENAMIC ACID; INSULIN; MECLOFENAMIC ACID; MEFENAMIC ACID; N (1,3 DIMETHYL 5 PYRAZOLYL)ANTHRANILIC ACID; NIFLUMIC ACID; S 645648; TOLFENAMIC ACID; TRANSIENT RECEPTOR POTENTIAL CHANNEL 6; TRANSIENT RECEPTOR POTENTIAL CHANNEL M2; TRANSIENT RECEPTOR POTENTIAL CHANNEL M3; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 4;

ARTICLE; CALCIUM CELL LEVEL; CELL MEMBRANE POTENTIAL; CELL STRAIN; CELL STRAIN HEK293; CELL STRAIN INS 1E; CONTROLLED STUDY; CYTOSOL; DRUG POTENCY; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; INSULIN RELEASE; PRIORITY JOURNAL; PROTEIN EXPRESSION; RECEPTOR BLOCKING;

ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; CALCIUM; FENAMATES; HEK293 CELLS; HUMANS; INSULIN; INSULIN-SECRETING CELLS; MEFENAMIC ACID; MICE; TRPC CATION CHANNELS; TRPM CATION CHANNELS; TRPV CATION CHANNELS;

EID: 79953052659     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2010.01186.x     Document Type: Article

References (60)

1. 2+ influx and its inhibition by N-(p-amylcinnamoyl)anthranilic acid in the beta-cells: involvement of TRPM2 channels. J Cell Mol Med 13: 3260-3267.
2. Beech DJ, Bahnasi YM, Dedman AM, Al-Shawaf E, (2009). TRPC channel lipid specificity and mechanisms of lipid regulation. Cell Calcium 45: 583-588.
3. Casas S, Novials A, Reimann F, Gomis R, Gribble FM, (2008). Calcium elevation in mouse pancreatic beta cells evoked by extracellular human islet amyloid polypeptide involves activation of the mechanosensitive ion channel TRPV4. Diabetologia 51: 2252-2262.
4. Caspani O, Heppenstall PA, (2009). TRPA1 and cold transduction: an unresolved issue? J Gen Physiol 133: 245-249.
5. Clapham DE, Julius D, Montell C, Schultz G, (2005). International Union of Pharmacology. XLIX. Nomenclature and structure-function relationships of transient receptor potential channels. Pharmacol Rev 57: 427-450. (Pubitemid 43036433)
6. Cryer B, Feldman M, (1998). Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs. Am J Med 104: 413-421. (Pubitemid 28274844)
7. Delmas P, (2005). Polycystins: polymodal receptor/ion-channel cellular sensors. Pflügers Arch 451: 264-276. (Pubitemid 41424931)
8. - channels contribute to volume regulation and phagocytosis in microglia. Eur J Neurosci 26: 2119-2130. (Pubitemid 47620476)
9. Dvorzhak AY, (2008). Effects of fenamate on inhibitory postsynaptic currents in Purkinje's cells. Bull Exp Biol Med 145: 564-568.
10. Fujimoto W, Miki T, Ogura T, Zhang M, Seino Y, Satin LS, et al,. (2009). Niflumic acid-sensitive ion channels play an important role in the induction of glucose-stimulated insulin secretion by cyclic AMP in mice. Diabetologia 52: 863-872.
11. Gögelein H, Pfannmüller B, (1989). The nonselective cation channel in the basolateral membrane of rat exocrine pancreas. Inhibition by 3′,5-dichlorodiphenylamine-2-carboxylic acid (DCDPC) and activation by stilbene disulfonates. Pflügers Arch 413: 287-298. (Pubitemid 19031571)
12. Gögelein H, Dahlem D, Englert HC, Lang HJ, (1990). Flufenamic acid, mefenamic acid and niflumic acid inhibit single nonselective cation channels in the rat exocrine pancreas. FEBS Lett 268: 79-82. (Pubitemid 20233835)
13. Grimm C, Kraft R, Sauerbruch S, Schultz G, Harteneck C, (2003). Molecular and functional characterization of the melastatin-related cation channel TRPM3. J Biol Chem 278: 21493-21501. (Pubitemid 36792546)
14. Guilbert A, Gautier M, Dhennin-Duthille I, Haren N, Sevestre H, Ouadid-Ahidouch H, (2009). Evidence that TRPM7 is required for breast cancer cell proliferation. Am J Physiol Cell Physiol 297: C493-C502.
15. 2+-activated non-selective cation channel in human atrial cardiomyocytes. J Physiol 558: 75-83. (Pubitemid 39077392)
16. Habjan S, Vandenberg RJ, (2009). Modulation of glutamate and glycine transporters by niflumic, flufenamic and mefenamic acids. Neurochem Res 34: 1738-1747.
17. Han JH, Bai GY, Park JH, Yuan K, Park WH, Kim SZ, et al,. (2008). Regulation of stretch-activated ANP secretion by chloride channels. Peptides 29: 613-621.
18. 2+-permeable channel activated by changes in redox status confers susceptibility to cell death. Mol Cell 9: 163-173. (Pubitemid 34127780)
19. Harteneck C, (2005). Function and pharmacology of TRPM cation channels. Naunyn Schmiedebergs Arch Pharmacol 371: 307-314. (Pubitemid 40905085)
20. Harteneck C, Plant TD, Schultz G, (2000). From worm to man: three subfamilies of TRP channels. Trends Neurosci 23: 159-166. (Pubitemid 30151212)
21. 2 inhibitor and TRP channel blocker. Cardiovasc Drug Rev 25: 61-75. (Pubitemid 46628622)
22. Hartmannsgruber V, Heyken WT, Kacik M, Kaistha A, Grgic I, Harteneck C, et al,. (2007). Arterial response to shear stress critically depends on endothelial TRPV4 expression. PLoS ONE 2: e827.
23. Hill K, Benham CD, McNulty S, Randall AD, (2004). Flufenamic acid is a pH-dependent antagonist of TRPM2 channels. Neuropharmacology 47: 450-460. (Pubitemid 38953236)
24. Hoffmann A, Grimm C, Kraft R, Goldbaum O, Wrede A, Nolte C, et al,. (2010). TRPM3 is expressed in sphingosine-responsive myelinating oligodendrocytes. J Neurochem 114: 654-665.
25. Huber TB, Schermer B, Müller RU, Höhne M, Bartram M, Calixto A, et al,. (2006). Podocin and MEC-2 bind cholesterol to regulate the activity of associated ion channels. Proc Natl Acad Sci USA 103: 17079-17086. (Pubitemid 44788925)
26. - channel function and cell volume regulation in AGS cells. Am J Physiol Gastrointest Liver Physiol 285: G938-G948. (Pubitemid 37310073)
27. Jordt SE, Julius D, (2002). Molecular basis for species-specific sensitivity to 'hot' chili peppers. Cell 108: 421-430. (Pubitemid 34178405)
28. Kankaanranta H, Moilanen E, (1995). Flufenamic and tolfenamic acids inhibit calcium influx in human polymorphonuclear leukocytes. Mol Pharmacol 47: 1006-1013.
29. Kraft R, Harteneck C, (2005). The mammalian melastatin-related transient receptor potential cation channels: an overview. Pflügers Arch 451: 204-211. (Pubitemid 41424924)
30. Kraft R, Grimm C, Frenzel H, Harteneck C, (2006). Inhibition of TRPM2 cation channels by N-(p-amylcinnamoyl)anthranilic acid. Br J Pharmacol 148: 264-273. (Pubitemid 43801173)
31. Lambert S, Oberwinkler J, (2005). Characterization of a proton-activated, outwardly rectifying anion channel. J Physiol 567: 191-213. (Pubitemid 41167315)
32. 2+-release channel in beta cells. Sci Signal 2: ra23.
33. Lee YM, Kim BJ, Kim HJ, Yang DK, Zhu MH, Lee KP, et al,. (2003). TRPC5 as a candidate for the nonselective cation channel activated by muscarinic stimulation in murine stomach. Am J Physiol Gastrointest Liver Physiol 284: G604-G616. (Pubitemid 36343210)
34. Leuner K, Kazanski V, Müller M, Essin K, Henke B, Gollasch M, et al,. (2007). Hyperforin-a key constituent of St. John's wort specifically activates TRPC6 channels. FASEB J 21: 4101-4111. (Pubitemid 350232367)
35. Leuner K, Heiser JH, Derksen S, Mladenov MI, Fehske CJ, Schubert R, et al,. (2010). Simple 2,4 diacylphloroglucinols as TRPC6 activators-identification of a novel pharmacophore. Mol Pharmacol 77: 368-377.
36. Li J, Zhang N, Ye B, Ju W, Orser B, Fox JE, et al,. (2007). Non-steroidal anti-inflammatory drugs increase insulin release from beta cells by inhibiting ATP-sensitive potassium channels. Br J Pharmacol 151: 483-493. (Pubitemid 46905011)
37. Montell C, Rubin GM, (1989). Molecular characterization of the Drosophila trp locus: a putative integral membrane protein required for phototransduction. Neuron 2: 1313-1323.
38. Montell C, Birnbaumer L, Flockerzi V, Bindels RJ, Bruford EA, Caterina MJ, et al,. (2002). A unified nomenclature for the superfamily of TRP cation channels. Mol Cell 9: 229-231. (Pubitemid 34195549)
39. Moreland JG, Davis AP, Bailey G, Nauseef WM, Lamb FS, (2006). Anion channels, including ClC-3, are required for normal neutrophil oxidative function, phagocytosis, and transendothelial migration. J Biol Chem 281: 12277-12288. (Pubitemid 43855312)
40. Müller M, Essin K, Hill K, Beschmann H, Rubant S, Schempp CM, et al,. (2008). Specific TRPC6 channel activation, a novel approach to stimulate keratinocyte differentiation. J Biol Chem 283: 33942-33954.
41. Numata T, Wehner F, Okada Y, (2007). A novel inhibitor of hypertonicity-induced cation channels in HeLa cells. J Physiol Sci 57: 249-252. (Pubitemid 350133541)
42. Parkerson KA, Sontheimer H, (2003). Contribution of chloride channels to volume regulation of cortical astrocytes. Am J Physiol Cell Physiol 284: C1460-C1467. (Pubitemid 36583387)
43. i. Proc Natl Acad Sci USA 100: 15166-15171. (Pubitemid 37518034)
44. Puertollano R, Kiselyov K, (2009). TRPMLs: in sickness and in health. Am J Physiol Renal Physiol 296: F1245-F1254.
45. Qian F, Huang P, Ma L, Kuznetsov A, Tamarina N, Philipson LH, (2002). TRP genes: candidates for nonselective cation channels and store-operated channels in insulin-secreting cells. Diabetes 51 (Suppl. 1): S183-S189. (Pubitemid 34761515)
46. + sensory neurons control β cell stress and islet inflammation in autoimmune diabetes. Cell 127: 1123-1135. (Pubitemid 44894522)
47. Reiser J, Polu KR, Moller CC, Kenlan P, Altintas MM, Wei C, et al,. (2005). TRPC6 is a glomerular slit diaphragm-associated channel required for normal renal function. Nat Genet 37: 739-744. (Pubitemid 41754891)
48. Reiter B, Kraft R, Günzel D, Zeissig S, Schulzke JD, Fromm M, et al,. (2006). TRPV4-mediated regulation of epithelial permeability. FASEB J 20: 1802-1812. (Pubitemid 44933794)
49. i oscillations in transgenically derived beta-cells. J Biol Chem 273: 10402-10410. (Pubitemid 28227649)
50. Sakura H, Ashcroft FM, (1997). Identification of four trp1 gene variants murine pancreatic beta-cells. Diabetologia 40: 528-532. (Pubitemid 27186788)
51. Talavera K, Nilius B, Voets T, (2008). Neuronal TRP channels: thermometers, pathfinders and life-savers. Trends Neurosci 31: 287-295.
52. 2+ channel in PC12 cells (an adrenal chromaffin cell line) correlates with expression of the TRP-6 (transient receptor potential) protein. Biochem J 358: 717-726. (Pubitemid 32896959)
53. Togashi K, Hara Y, Tominaga T, Higashi T, Konishi Y, Mori Y, et al,. (2006). TRPM2 activation by cyclic ADP-ribose at body temperature is involved in insulin secretion. EMBO J 25: 1804-1815.
54. Ullrich S, Berchtold S, Ranta F, Seebohm G, Henke G, Lupescu A, et al,. (2005). Serum- and glucocorticoid-inducible kinase 1 (SGK1) mediates glucocorticoid-induced inhibition of insulin secretion. Diabetes 54: 1090-1099. (Pubitemid 40446323)
55. Vennekens R, Owsianik G, Nilius B, (2008). Vanilloid transient receptor potential cation channels: an overview. Curr Pharm Des 14: 18-31. (Pubitemid 351266981)
56. Vietri M, De Santi C, Pietrabissa A, Mosca F, Pacifici GM, (2000). Fenamates and the potent inhibition of human liver phenol sulphotransferase. Xenobiotica 30: 111-116. (Pubitemid 30125112)
57. Vriens J, Appendino G, Nilius B, (2009). Pharmacology of vanilloid transient receptor potential cation channels. Mol Pharmacol 75: 1262-1279.
58. Wagner TF, Loch S, Lambert S, Straub I, Mannebach S, Mathar I, et al,. (2008). Transient receptor potential M3 channels are ionotropic steroid receptors in pancreatic beta cells. Nat Cell Biol 10: 1421-1430.
59. Watanabe H, Davis JB, Smart D, Jerman JC, Smith GD, Hayes P, et al,. (2002). Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives. J Biol Chem 277: 13569-13577. (Pubitemid 34967954)
60. Wehrhahn J, Kraft R, Harteneck C, Hauschildt S, (2010). Transient receptor potential melastatin 2 is required for lipopolysaccharide-induced cytokine production in human monocytes. J Immunol 184: 2386-2393.