Transient receptor potential channels as drug targets

Expert Opinion on Therapeutic Targets

Volumn 11, Issue 3, 2007, Pages 391-401

  Okuhara, Dayne Y ^a   Hsia, Albert Y ^a   Xie, Michael ^a,b  

^a Synta Pharmaceuticals Corp   (United States)

^b Epix Pharmaceuticals   (United States)

Author keywords

Ion channel; Non selective cation channel; Transient receptor potential; TRP

Indexed keywords

AGENTS AFFECTING PROTEIN METABOLISM; BETA ADRENERGIC RECEPTOR STIMULATING AGENT; CATION CHANNEL; CORTICOSTEROID; ION CHANNEL; MELASTATIN; POLYCYSTIN 1; TRANSIENT RECEPTOR POTENTIAL A PROTEIN; TRANSIENT RECEPTOR POTENTIAL C1 PROTEIN; TRANSIENT RECEPTOR POTENTIAL C3 PROTEIN; TRANSIENT RECEPTOR POTENTIAL C6 PROTEIN; TRANSIENT RECEPTOR POTENTIAL C6 PROTEIN INHIBITOR; TRANSIENT RECEPTOR POTENTIAL M2 PROTEIN; TRANSIENT RECEPTOR POTENTIAL M3 PROTEIN; TRANSIENT RECEPTOR POTENTIAL M4 PROTEIN; TRANSIENT RECEPTOR POTENTIAL M5 PROTEIN; TRANSIENT RECEPTOR POTENTIAL M6 PROTEIN; TRANSIENT RECEPTOR POTENTIAL M7 PROTEIN; TRANSIENT RECEPTOR POTENTIAL M8 PROTEIN; TRANSIENT RECEPTOR POTENTIAL ML PROTEIN; TRANSIENT RECEPTOR POTENTIAL P PROTEIN; TRANSIENT RECEPTOR POTENTIAL P2 PROTEIN ACTIVATOR; TRANSIENT RECEPTOR POTENTIAL PROTEIN; TRANSIENT RECEPTOR POTENTIAL V1 PROTEIN; TRANSIENT RECEPTOR POTENTIAL V2 PROTEIN; TRANSIENT RECEPTOR POTENTIAL V3 PROTEIN; TRANSIENT RECEPTOR POTENTIAL V4 PROTEIN; TRANSIENT RECEPTOR POTENTIAL V5 PROTEIN; TRANSIENT RECEPTOR POTENTIAL V6 PROTEIN; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ASTHMA; BLOOD VESSEL TONE; CANCER; CELL STIMULATION; CHANNELOPATHY; CHRONIC OBSTRUCTIVE LUNG DISEASE; CLINICAL TRIAL; DRUG INDUSTRY; DRUG RESEARCH; DRUG TARGETING; HUMAN; INCONTINENCE; MICTURITION; MIGRAINE; NEURALGIA; NEUROPATHY; NONHUMAN; PAIN; PRODUCT DEVELOPMENT; PROTEIN EXPRESSION; PROTEIN FAMILY; PROTEIN FUNCTION; PROTEIN TARGETING; REVIEW; SENSORY STIMULATION; TEMPERATURE SENSE; TOOTH PAIN;

ANIMALS; CENTRAL NERVOUS SYSTEM; DRUG DESIGN; ENDOTHELIAL CELLS; HUMANS; MYOCYTES, SMOOTH MUSCLE; TRANSIENT RECEPTOR POTENTIAL CHANNELS;

EID: 33847156838     PISSN: 14728222     EISSN: None     Source Type: Journal    
DOI: 10.1517/14728222.11.3.391     Document Type: Review

References (99)

1. ASHCROFT FM: From molecule to malady. Nature (2006) 440:440-447.
2. 2+ channel in Drosophila photoreceptors. Neuron (1992) 8:643-651.
3. MONTELL C: The TRP superfamily of cation channels. Sci. STKE (2005) 2005:re3.
4. RAMSEY IS, DELLING M, CLAPHAM DE: An introduction to TRP channels. Ann. Rev. Physiol. (2006) 68:619-647.
5. FREICHEL M, VENNEKENS R, OLAUSSON J et al.: Functional role of TRPC proteins in native systems: implications from knockout and knock-down studies. J. Physiol. (2005) 567:59-66.
6. LI S, GOSLING M, POLL C: Determining the functional role of TRPC channels in primary cells. Pflugers Arch. (2005) 451:43-52.
7. NILIUS B, VOETS T, PETERS J: TRP channels in disease. Sci. STKE (2005) 2005:re8.
8. LIMAN ER, INNAN H: Relaxed selective pressure on an essential component of pheromone transduction in primate evolution. Proc. Natl. Acad. Sci. USA (2003) 100:3328-3332.
9. 2+ in pulmonary arterial smooth muscle cells. Circ. Res. (2006) 98:1528-1537.
10. YAO X, GARLAND CJ: Recent developments in vascular endothelial cell transient receptor potential channels. Circ. Res. (2005) 97:853-863.
11. 2+ channels in pulmonary arterial smooth muscle cells: a novel mechanism of hypoxic pulmonary hypertension. Circ. Res. (2004) 95:496-505.
12. 2+ influx. Circ. Res. (2005) 96:1282-1290.
13. MORAN MM, XU H, CLAPHAM DE: TRP ion channels in the nervous system. Curr. Opin. Neurobiol. (2004) 14:362-369.
14. KIM SJ, KIM YS, YUAN JP, PETRALIA RS, WORLEY PF, LINDEN DJ: Activation of the TRPC1 cation channel by metabotropic glutamate receptor mGluR1. Nature (2003) 426:285-291.
15. KWAN HY, HUANG Y, YAO X: Regulation of canonical transient receptor potential isoform 3 (TRPC3) channel by protein kinase G. Proc. Natl. Acad. Sci. USA (2004) 101:2625-2630.
16. VENKATACHALAM K, ZHENG F, GILL DL: Regulation of canonical transient receptor potential (TRPC) channel function by diacylglycerol and protein kinase C. J. Biol. Chem. (2003) 278:29031-29040.
17. SHI J, MORI E, MORI Y et al.: Multiple regulation by calcium of murine homologues of transient receptor potential proteins TRPC6 and TRPC7 expressed in HEK293 cells. J. Physiol. (2004) 561:415-432.
18. READING SA, EARLEY S, WALDRON BJ, WELSH DG, BRAYDEN JE: TRPC3 mediates pyrimidine receptor-induced depolarization of cerebral arteries. Am. J. Physiol. Heart Circ. Physiol. (2005) 288:H2055-H2061.
19. KAMOUCHI M, PHILIPP S, FLOCKERZI V et al.: Properties of heterologously expressed hTRP3 channels in bovine pulmonary artery endothelial cells. J. Physiol. (1999) 518(Pt. 2):345-358.
20. LI Y, JIA YC, CUI K, LI N, ZHENG ZY, WANG YZ, YUAN XB: Essential role of TRPC channels in the guidance of nerve growth cones by brain-derived neurotrophic factor. Nature (2005) 434:894-898.
21. BALZER M, LINTSCHINGER B, GROSCHNER K: Evidence for a role of Trp proteins in the oxidative stress-induced membrane conductances of porcine aortic endothelial cells. Cardiovasc. Res. (1999) 42:543-549.
22. MILLER BA: The role of TRP channels in oxidative stress-induced cell death. J. Membr. Biol. (2006) 209:31-41.
23. POTESER M, GRAZIANI A, ROSKER C et al.: TRPC3 and TRPC4 associate to form a redox-sensitive cation channel. Evidence for expression of native TRPC3-TRPC4 heteromeric channels in endothelial cells. J. Biol. Chem. (2006) 281:13588-13595.
24. 2+ entry via NCX reversal in ATP stimulated smooth muscle cells. Biochem. Biophys. Res. Commun. (2006) 352:130-134.
25. EDER P, PROBST D, ROSKER C, POTESER M et al.: Phospholipase C-dependent control of cardiac calcium homeostasis involves a TRPC3-NCX1 signaling complex. Cardiovasc. Res. (2006) In Press.
26. HASSOCK SR, ZHU MX, TROST C, FLOCKERZI V, AUTHI KS: Expression and role of TRPC proteins in human platelets: evidence that TRPC6 forms the store-independent calcium entry channel. Blood (2002) 100:2801-2811.
27. INOUE R, JENSEN LJ, SHI J et al.: Transient receptor potential channels in cardiovascular function and disease. Circ. Res. (2006) 99:119-131.
28. YU Y, FANTOZZI I, REMILLARD CV et al.: Enhanced expression of transient receptor potential channels in idiopathic pulmonary arterial hypertension. Proc. Natl. Acad. Sci. USA (2004) 101:13861-13866.
29. WELSH DG, MORIELLI AD, NELSON MT, BRAYDEN JE: Transient receptor potential channels regulate myogenic tone of resistance arteries. Circ. Res. (2002) 90:248-250.
30. WINN MP, CONLON PJ, LYNN KL et al.: A mutation in the TRPC6 cation channel causes familial focal segmental glomerulosclerosis. Science (2005) 308:1801-1804.
31. REISER J, POLU KR, MOLLER CC et al.: TRPC6 is a glomerular slit diaphragm-associated channel required for normal renal function. Nat. Genet. (2005) 37:739-744.
32. DIETRICH A, CHUBANOV V, KALWA H, ROST BR, GUDERMANN T: Cation channels of the transient receptor potential superfamily: their role in physiological and pathophysiological processes of smooth muscle cells. Pharmacol. Ther. (2006) 112:744-760.
33. VAZQUEZ G, BIRD GS, MORI Y, PUTNEY JW JR: Native TRPC7 channel activation by an inositol trisphosphate receptor-dependent mechanism. J. Biol. Chem. (2006) 281:25250-25258.
34. STRUBING C, KRAPIVINSKY G, KRAPIVINSKY L, CLAPHAM DE: TRPC1 and TRPC5 form a novel cation channel in mammalian brain. Neuron (2001) 29:645-655.
35. MUNSCH T, FREICHEL M, FLOCKERZI V, PAPE HC: Contribution of transient receptor potential channels to the control of GABA release from dendrites. Proc. Natl. Acad. Sci. USA (2003) 100:16065-16070.
36. 2+ current impairs agonist-dependent vasorelaxation in TRP4-/- mice. Nat. Cell. Biol. (2001) 3:121-127.
37. 2+ entry in TRPC4(-/-) mice interferes with increase in lung microvascular permeability. Circ. Res. (2002) 91:70-76.
38. GREKA A, NAVARRO B, OANCEA E, DUGGAN A, CLAPHAM DE: TRPC5 is a regulator of hippocampal neurite length and growth cone morphology. Nat. Neurosci. (2003) 6:837-845.
39. CATERINA MJ, SCHUMACHER MA, TOMINAGA M, ROSEN TA, LEVINE JD, JULIUS D: The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature (1997) 389:816-824.
40. LEE H, CATERINA MJ: TRPV channels as thermosensory receptors in epithelial cells. Pflugers Arch. (2005) 451:160-167.
41. BARTON NJ, MCQUEEN DS, THOMSON D et al.: Attenuation of experimental arthritis in TRPV1R knockout mice. Exp. Mol. Pathol. (2006) 81:166-170.
42. AVELINO A, CRUZ F: TRPV1 (vanilloid receptor) in the urinary tract: expression, function and clinical applications. Naunyn Schmiedebergs Arch. Pharmacol. (2006) 373:287-299.
43. WANG LH, LUO M, WANG Y, GALLIGAN JJ, WANG DH: Impaired vasodilation in response to perivascular nerve stimulation in mesenteric arteries of TRPV1-null mutant mice. J. Hypertens. (2006) 24:2399-2408.
44. MURAKI K, IWATA Y, KATANOSAKA Y et al.: TRPV2 is a component of osmotically sensitive cation channels in murine aortic myocytes. Circ. Res. (2003) 93:829-838.
45. MOQRICH A, HWANG SW, EARLEY TJ et al.: Impaired thermosensation in mice lacking TRPV3, a heat and camphor sensor in the skin. Science (2005) 307:1468-1472.
46. CHUNG MK, LEE H, MIZUNO A, SUZUKI M, CATERINA MJ: TRPV3 and TRPV4 mediate warmth-evoked currents in primary mouse keratinocytes. J. Biol. Chem. (2004) 279:21569-21575.
47. + secretion from the cortical collecting duct. Am. J. Physiol. Renal Physiol. (2006) In Press.
48. HOENDEROP JG, NILIUS B, BINDELS RJ: Calcium absorption across epithelia. Physiol. Rev. (2005) 85:373-422.
49. BIANCO SD, PENG JB, TAKANAGA H et al.: Marked disturbance of calcium homeostasis in mice with targeted disruption of the trpv6 calcium channel gene. J. Bone. Miner. Res. (2006) In Press.
50. 2+ channel expression. Biochem. Biophys. Res. Commun. (2004) 322:1359-1363.
51. FONFRIA E, MURDOCK PR, CUSDIN FS, BENHAM CD, KELSELL RE, MCNULTY S: Tissue distribution profiles of the human TRPM cation channel family. J. Recept. Signal Transduct. Res. (2006) 26:159-178.
52. DUNCAN LM, DEEDS J, HUNTER J et al.: Down-regulation of the novel gene melastatin correlates with potential for melanoma metastasis. Cancer Res. (1998) 58:1515-1520.
53. HARTENECK C: Function and pharmacology of TRPM cation channels. Naunyn Schmiedebergs Arch. Pharmacol. (2005) 371:307-314.
54. 2+-activated non-selective cation channel mediating cell membrane depolarization. Cell (2002) 109:397-407.
55. FARLEY S, WALDRON BJ, BRAYDEN JE: Critical role for transient receptor potential channel TRPM4 in myogenic constriction of cerebral arteries. Circ. Res. (2004) 95:922-929.
56. CHENG H, BECK A, LAUNAY P et al.: TRPM4 controls insulin secretion in pancreatic beta-cells. Cell Calcium (2006) 41:51-61.
57. LAUNAY P, CHENG H, SRIVATSAN S, PENNER R, FLEIG A, KINET JP: TRPM4 regulates calcium oscillations after T cell activation. Science (2004) 306:1374-1377.
58. 2+-activated monovalent selective cation channel. Curr. Biol. (2003) 13:1153-1158.
59. ZHANG Y, HOON MA, CHANDRASHEKAR J et al.: Coding of sweet, bitter, and umami tastes: different receptor cells sharing similar signaling pathways. Cell (2003) 112:293-301.
60. 2+ absorption. J. Biol. Chem. (2004) 279:19-25.
61. NADLER MJ, HERMOSURA MC, INABE K et al.: LTRPC7 is a Mg.ATP-regulated divalent cation channel required for cell viability. Nature (2001) 411:590-595.
62. SCHLINGMANN KP, WEBER S, PETERS M et al.: Hypomagnesemia with secondary hypocalcemia is caused by mutations in TRPM6, a new member of the TRPM gene family. Nat. Genet. (2002) 31:166-170.
63. WALDER RY, LANDAU D, MEYER P et al.: Mutation of TRPM6 causes familial hypomagnesemia with secondary hypocalcemia. Nat. Genet. (2002) 31:171-174.
64. AARTS M, IIHARA K, WEI WL et al.: A key role for TRPM7 channels in anoxic neuronal death. Cell (2003) 115:863-877.
65. BECK A, KOLISEK M, BAGLEY LA, FLEIG A, PENNER R: Nicotinic acid adenine dinucleotide phosphate and cyclic ADP-ribose regulate TRPM2 channels in T lymphocytes. FASEB J. (2006) 20:962-964.
66. YANG KT, CHANG WL, YANG PC et al.: Activation of the transient receptor potential M2 channel and poly(ADP-ribose) polymerase is involved in oxidative stress-induced cardiomyocyte death. Cell Death Differ. (2006) 13:1815-1826.
67. BRAUCHI S, ORIO P, LATORRE R: Clues to understanding cold sensation: thermodynamics and electrophysiological analysis of the cold receptor TRPM8. Proc. Natl. Acad. Sci. USA (2004) 101:15494-15499.
68. SCHMIDT U, FUESSEL S, KOCH R et al.: Quantitative multi-gene expression profiling of primary prostate cancer. Prostate (2006) 66:1521-1534.
69. NAULI SM, ALENGHAT FJ, LUO Y et al.: Polycystins 1 and 2 mediate mechanosensation in the primary cilium of kidney cells. Nat. Genet. (2003) 33:129-137.
70. KOULEN P, CAI Y, GENG L et al.: Polycystin-2 is an intracellular calcium release channel. Nat. Cell Biol. (2002) 4:191-197.
71. IGARASHI P, SOMLO S: Genetics and pathogenesis of polycystic kidney disease. J. Am. Soc. Nephrol. (2002) 13:2384-2398.
72. YODER BK, HOU X, GUAY-WOODFORD LM: The polycystic kidney disease proteins, polycystin-1, polycystin-2, polaris, and cystin, are co-localized in renal cilia. J. Am. Soc. Nephrol. (2002) 13:2508-2516.
73. PRAETORIUS HA, SPRING KR: A physiological view of the primary cilium. Ann. Rev. Physiol. (2005) 67:515-529
74. MENE P: Transient receptor potential channels in the kidney: calcium signaling, transport and beyond. J. Nephrol. (2006) 19:21-29.
75. 2+ influx. Cell Struct. Funct. (2005) 30:93-100.
76. SIROKY BJ, FERGUSON WB, FUSON AL et al.: Loss of primary cilia results in deregulated and unabated apical calcium entry in ARPKD collecting duct cells. Am. J. Physiol. Renal Physiol. (2006) 290:F1320-F11328.
77. BASSI MT, MANZONI M, MONTI E, PIZZO MT, BALLABIO A, BORSANI G: Cloning of the gene encoding a novel integral membrane protein, mucolipidin-and identification of the two major founder mutations causing mucolipidosis Type IV. Am. J. Hum. Genet. (2000) 67:1110-1120.
78. SUN M, GOLDIN E, STAHL S et al.: Mucolipidosis Type IV is caused by mutations in a gene encoding a novel transient receptor potential channel. Hum. Mol. Genet. (2000) 9:2471-2478.
79. RAYCHOWDHURY MK, GONZALEZ-PERRETT S, MONTALBETTI N et al.: Molecular pathophysiology of mucolipidosis Type IV: pH dysregulation of the mucolipin-1 cation channel. Hum. Mol. Genet. (2004) 13:617-627.
80. STORY GM, PEIER AM, REEVE AJ et al.: ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures. Cell (2003) 112:819-829.
81. KWAN KY, ALLCHORNE AJ, VOLLRATH MA et al.: TRPA1 contributes to cold, mechanical, and chemical nociception but is not essential for hair-cell transduction. Neuron (2006) 50:277-289.
82. BAUTISTA DM, JORDT SE, NIKAI T et al.: TRPA1 mediates the inflammatory actions of environmental irritants and proalgesic agents. Cell (2006) 124:1269-1282.
83. NAGATA K, DUGGAN A, KUMAR G, GARCIA-ANOVEROS J: Nociceptor and hair cell transducer properties of TRPA1, a channel for pain and hearing. J. Neurosci. (2005) 25:4052-4061.
84. COREY DP, GARCIA-ANOVEROS J, HOLT JR et al.: TRPA1 is a candidate for the mechanosensitive transduction channel of vertebrate hair cells. Nature (2004) 432:723-730.
85. 2+ entry and attenuates pulmonary artery smooth muscle cell proliferation. Am. J. Physiol. Lung Cell. Mol. Physiol. (2002) 283:L144-L155.
86. BARNES PJ, HANSEL TT: Prospects for new drugs for chronic obstructive pulmonary disease. Lancet (2004) 364:985-996.
87. 2+ release from endoplasmic reticulum in B lymphocytes. J. Exp. Med. (2002) 195:673-681.
88. HIGASHI Y, NISHIOKA K, UMEMURA T, CHAYAMA K, YOSHIZUMI M: Oxidative stress, endothelial function and angiogenesis induced by cell therapy and gene therapy. Curr. Pharm. Biotechnol. (2006) 7:109-116.
89. 2+ channel required for the survival of prostate cancer cells. Cancer Res. (2004) 64:8365-8373.
90. HIANI YE, AHIDOUCH A, ROUDBARAKI M, GUENIN S, BRULE G, OUADID-AHIDOUCH H: Calcium-sensing receptor stimulation induces non-selective cation channel activation in breast cancer cells. J. Membr. Biol. (2006) 211:127-137.
91. 2+ oscillations by the calcium sensing receptor. J. Biol. Chem. (2006) 281:38730-38737.
92. MANNING AT, O'BRIEN N, KERIN MJ: Roles for the calcium sensing receptor in primary and metastatic cancer. Eur. J. Surg. Oncol. (2006) 32:693-697.
93. 2+ channel in renal microcirculation and glomeruli. Exp. Biol. Med. (2006) 231:145-153.
94. GOEL M, SINKINS WG, ZUO CD, ESTACION M, SCHILLING WP: Identification and localization of TRPC channels in the rat kidney. Am. J. Physiol. Renal Physiol. (2006) 290:F1241-F1252.
95. SZALLASI A, CRUZ F, GEPPETTI P: TRPV1: a therapeutic target for novel analgesic drugs? Trends Mol. Med. (2006) 12:545-554.
96. ALESSANDRI-HABERN, JOSEPH E, DINA OA, LIEDTKE W, LEVINE JD: TRPV4 mediates pain-related behavior induced by mild hypertonic stimuli in the presence of inflammatory mediator. Pain (2005) 118:70-79
97. ALESSANDRI-HABER N, YEH JJ, BOYD AE et al.: Hypotonicity induces TRPV4-mediated nociception in rat. Neuron (2003) 39:497-511.
98. BEECH DJ: TRPC1: store-operated channel and more. Pflugers Arch. (2005) 451:53-60.
99. SANDERS JL, CHATTOPADHYAY N, KIFOR O, YAMAGUCHI T, BUTTERS RR, BROWN EM: Extracellular calcium-sensing receptor expression and its potential role in regulating parathyroid hormone-related peptide secretion in human breast cancer cell lines. Endocrinology (2000) 141:4357-4364.