Toxin modulators and blockers of hERG K + channels

Toxicon

Volumn 60, Issue 4, 2012, Pages 492-501

  Jimenez Vargas J M ^a   Restano Cassulini, R ^a   Possani, L D ^a  

^a INSTITUTO DE BIOTECNOLOGÍA   (Mexico)

Author keywords

Anemone; Erg channel; K + channel; Scorpion; Spider; Toxin

Indexed keywords

POTASSIUM CHANNEL HERG; POTASSIUM CHANNEL HERG1; POTASSIUM CHANNEL HERG2; POTASSIUM CHANNEL HERG3; SCORPION VENOM; SEA ANEMONE TOXIN; SPIDER VENOM; UNCLASSIFIED DRUG; VOLTAGE GATED POTASSIUM CHANNEL;

ALPHA HELIX; AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ARTICLE; BETA SHEET; BINDING SITE; CHANNEL GATING; CONFORMATIONAL TRANSITION; HYDROPHOBICITY; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROTEIN PROTEIN INTERACTION; SEQUENCE ALIGNMENT; SURFACE PROPERTY;

AMINO ACID SEQUENCE; ANIMALS; CNIDARIAN VENOMS; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; ION CHANNEL GATING; MOLECULAR SEQUENCE DATA; POTASSIUM CHANNEL BLOCKERS; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; SCORPION VENOMS; SPECIES SPECIFICITY; SPIDER VENOMS; STRUCTURE-ACTIVITY RELATIONSHIP; VENOMS;

ACTINIARIA; ANEMONE; ANIMALIA; ARANEAE; SCORPIONES;

EID: 84863784895     PISSN: 00410101     EISSN: 18793150     Source Type: Journal    
DOI: 10.1016/j.toxicon.2012.03.024     Document Type: Article

References (98)

1. + channels. Biochem. Pharmacol. 2008, 76:805-815.
2. Akbarali H.K., Thatte H., He X.D., Giles W.R., Goyal R.K. Role of HERG-like K(+) currents in opossum esophageal circular smooth muscle. Am. J. Physiol. 1999, 277:C1284-C1290.
3. Alabi A.A., et al. Portability of paddle motif function and pharmacology in voltage sensors. Nature 2007, 450:370-375.
4. v channels. Biophys. J. 2006, 90:B287.
5. Al-Owais M., Bracey K., Wray D. Role of intracellular domains in the function of the herg potassium channel. Eur. Biophys. J. 2009, 38:569-576.
6. Anderson C.L., Delisle B.P., Andon B.D., Kilby J.A., Will M.L., Tester D.J. Most LQT2 mutations reduce Kv11.1 (hERG) current by a class 2 (trafficking-deficient) mechanism. Circulation 2006, 113:365-373.
7. Bauer C.K., Engeland B., Wulfsen I., Ludwing J., Pongs O., Schwarz J.R. RERG is amolecular correlate of the inward-rectifying K current in clonal rat pituitary cells. Receptor Channels 1998, 6:19-29.
8. Bosmans F., et al. Deconstructing voltage sensor function and pharmacology in sodium channels. Nature 2008, 456:203-208.
9. Chagot B., Diochot S., Pimentel C., Lazdunski M., Darbon H. Solution structure of APETx1 from the sea anemone Anthopleura elegantissima: a new fold for an HERG toxin. Proteins 2005, 59:380-386.
10. Chen J., Zou A., Splawski I., Keating M., Sanguinetti M.C. Long QT syndrome-associated mutations in the Per-Arnt-Sim (PAS) domain of HERG potassium channels accelerate channel deactivation. J. Biol. Chem. 1999, 274:10113-10118.
11. + channels. Proc. Natl. Acad. Sci. USA 1991, 88:5092-5095.
12. + channels. J. Physiol. 2006, 573:291-304.
13. Clement H., Odell G., Zamudio F.Z., Redaelli E., Wanke E., Alagón A., Possani L.D. Isolation and characterization of a novel toxin from the venom of the spider Grammostola rosea that blocks sodium channels. Toxicon 2007, 50:65-74.
14. +-channels blocking peptides from scorpions of the genus Centruroides. FEBS Lett. 2002, 532:121-126.
15. + channel blocker peptide isolated from the scorpion Centruroides limpidus limpidus. J. Braz. Chem. Soc. 2005, 16(3A):404-411.
16. Corrette B.J., Bauer C.K., Schwarz J.R. An inactivating inward-rectifying K current present in prolactin cells from the pituitary of lactating rats. J. Membr. Biol. 1996, 150:185-195.
17. Curran M.E., Splaswki I., Timothy K.W., Vicent G.M., Green E.D., Keating M.T. A molecular bases for cardiac arrhythmia: HERG mutations cause long QT syndrome. Cell 1995, 80(5):795-803.
18. Diochot S., Loret E., Bruhn T., Beress L., Lazdunski M. APETx1, a new toxin from the sea anemone Anthopleura elegantissima, blocks voltage-gated human ether-a-go-go-related gene potassium channels. Mol. Pharmacol. 2003, 64:59-69.
19. + conduction and selectivity. Science 1998, 280:69-77.
20. + channels. Proteins 2004, 56:367-375.
21. García M.L., et al. Potassium channels: from scorpion venoms to high-resolution structure. Toxicon 2001, 39:739-748.
22. Guasti L., Cilia E., Crociani O., Hofmann G., Polvani S., Becchetti A., Wanke E., Tempia F., Arcangeli A. Expression pattern of the ether-à -go-go-related (ERG) family proteins in the adult mouse central nervous system: evidence for coassembly of different subunits. J. Comp. Neurol. 2005, 491:157-174.
23. + cannel blockade enhances firing and epinephrine secretion in rat chromaffin cells: the missing link to LQT2-related sudden death?. FASEB J. 2003, 17:330-332.
24. + channels isolated from Centruroides noxius scorpion venom. FASEB J. 1999, 13:953-962.
25. Hill A.P., Campbell T.J., Bansal P.S., Kuchel P.W., Vandenberg J.I. The S631A mutation causes a mechanistic switch in the block of hERG channels by CnErg1. Biophys. J. 2007, 32-34.
26. + channel by the scorpion toxin CnErg1. Biophys. J. 2007, 92:3915-3929.
27. + channels: effects of alterations in the carboxy-terminal region. Neuron 1991, 7:547-556.
28. Huang P.T., Shiau Y.S., Lou K.L. The interaction of spider gating modifier peptides with voltage-gated potassium channels. Toxicon 2007, 49(2):285-292.
29. + and HERG currents. Biochem. J. 2004, 378:745-752.
30. Jiang C., Atkinson D., Towbin J., Splawski I., Lehmann M., Li H., Timothy K., Taggart T., Schwartz P., Vincent G. Two long QT syndrome loci map to chromosome 3 and 7 with evidence for further heterogeneity. Nat. Genet. 1994, 8:141-147.
31. + channel. Nature 2003, 423:42-48.
32. Jiménez-Vargas J.M., Restano-Cassulini R., Quintero-Hernández V., Gurrola G.B., Possani L.D. Recombinant expression of the toxin peptide ErgTx1 and role of Met35 on its stability and function. Peptides 2011, 32:560-567.
33. + channels. Toxicon 2012, 59:633-641.
34. Jung H.J., Kim P.I., Lee S.K., Lee C.W., Eu Y.J., Lee D.G., Earm Y.E., Kim J.I. Biochem. Biophys. Res. Commun. 2006, 340:633-638.
35. King G.F., Gentz M.C., Escoubas P., Nicholson G.M. A rational nomenclature for naming peptide toxins from spiders and other venomous animals. Toxicon 2008, 52:264-276.
36. Korolkova Y.V., Bocharov E.V., Angelo K., Maslennikov I.V., Grinenko O.V., Lipkin A.V., Nosyreva E.D., Pluzhnikov K.A., Olesen S.P., Arseniev A.S., Grishin E.V. New binding site on common molecular scaffold provides HERG channel specificity of scorpion toxin BeKm-1. J. Biol. Chem. 2002, 277:43104-43109.
37. Korolkova Y.V., Kozlov S.A., Lipkin A.V., Pluzhnikov K.A., Hardley J.K., Filippov A.K., Brown D.A., Angelo K., Strobaek D., Jespersen T., Olesen S.P., Jensen B.S., Grishin E.V. An ERG channel inhibitor from the scorpion Buthus eupeus. J. Biol. Chem. 2001, 276:9868-9876.
38. Korolokova Y.V., Tseng G.N., Grishin E.V. Unique interaction of scorpion toxins with the hERG channel. J. Mol. Recognit. 2004, 17:209-217.
39. Kozlov S., Grishin E. Convenient nomenclature of cysteine-rich polypeptide toxins from sea anemones. Peptides 2012, 33:240-244.
40. Lampe R.A. Analgesic Peptides from Venom of Grammostola spatula and Use Thereof 1999, US Patent: 5,877,026.
41. Lampe R.A., Sanchs F. US Patent: 5968838 1999.
42. + current in MMQ lactotrophs and its accommodating role during slow firing and prolactin release. J. Neurosci. 2002, 22:3414-3425.
43. Lee C.W., Kim S., Roh S.H., Endoh H., Kodera Y., Maeda T., Kohno T., Wang J.M., Swartz K.J., Kim J.I. Solution structure and functional characterization of SGTx1, a modifier of Kv2.1 channel gating. Biochemistry 2004, 43:890-897.
44. Lee S.Y., Mackinnon R. A membrane-access mechanism of ion channel inhibition by voltage sensor toxins from spider venom. Nature 2004, 430:232-235.
45. + channel in mouse and human hearts. Circ. Res. 1997, 81:719-726.
46. + channel during gating. Neuron 2000, 16:859-867.
47. Liu J., Zhang M., Jiang M., Tseng G.N. Structural and functional role of the extracellular S5-P linker in the HERG potassium channel. J. Gen. Physiol. 2002, 120:723-737.
48. Liu J., Zhang M., Jiang M., Tseng G.N. Negative charges in the transmembrane domains of the HERG K channel are involved in the activation-and deactivation gating processes. J. Gen. Physiol. 2003, 121:599-614.
49. Liu S., Rasmusson R.C., Campbell D.C., Wang S., Strauss H.C. Activation and inactivation kinetics of an E-4031-sensitive current from single ferret atrial myocytes. Biophys. J. 1996, 70:2704-2715.
50. + current. Circ. Res. 1997, 81:870-878.
51. Milescu M., Bosmans F., Lee S., Alabi A.A., Kim J.I., Swartz K.J., et al. Interactions between lipids and voltage sensors paddles detected with tarantula toxins. Nat. Struct. Mol. Biol. 2009, 16:1080-1085.
52. Milnes J.T., Dempsey C.E., Ridley J.M., Crociani O., Arcangeli A., Hancox J.C., Witchel H.J. Preferential closed channel blockade of HERG potassium currents by chemically synthetized BeKm-1 scorpion toxin. FEBS Lett. 2003, 547:20-26.
53. Morais-Cabral J.H., Lee A., Cohen S.L., Chait B.T., Li M., Mackinnon R. Crystal structure and functional analysis of the HERG potassium channel N terminus: a eukaryotic PAS domain. Cell 1998, 95:649-655.
54. Nastainczyk W., Meves H., Watt D.D. A short-chain peptide toxin isolated from Centruroides sculpturatus scorpion venom inhibits ether-a-go-go-related gene K(+) channels. Toxicon 2002, 40:1053-1058.
55. Oswald R.E., Suchyna T.M., McFeeters R., Gottlieb P., Sachs F. Solution structure of peptides toxins that block mechanosensitive ion channels. J. Biol. Chem. 2002, 277:34443-34450.
56. Overholt J.L., Ficker E., Yang T., Shams H., Bright G.R., Prabhakar N.R. HERG-like potassium current regulates the resting membrane potential in glomus cells of the rabbit carotid body. J. Neurophysiol. 2000, 83:1150-1157.
57. Papa M., Boscia F., Canitano A., Castaldo P., Sellitti S., Annunziato L., Taglialatela M. Expression pattern of the ether-à -gogo-related (ERG) K+ channel encoding genes ERG1, ERG2, and ERG3 in the adult rat central nervous system. J. Comp. Neurol. 2003, 466:119-135.
58. Pardo-López L., García-Valdés J., Gurrola G.B., Robertson G.A., Possani L.D. Mapping the receptor site for ergtoxin, a specific blocker of ERG channels. FEBS Lett. 2002, 510:45-49.
59. Pardo-López L., Zhang M., Liu J., Jiang M., Possani L.D., Tseng G.N. Mapping the binding site of a human ether-a-go-go-related gene-specific peptide toxin (ErgTx) to the channel's outer vestibule. J. Biol. Chem. 2002, 277:16403-16411.
60. Phillips L.R., Milescu M., Li-Smerin Y., Mindell J.A., Kim J.I., Swartz K.J. Voltage-sensor activation with a tarantula toxin as cargo. Nature 2005, 436:857-860.
61. Piper D.R., Hinz W.A., Tallurri C.K., Sanguinetti M.C., Tristani-Firuouzi M. Regional specificity of hERG channel activation and inactivation gating. J. Biol. Chem. 2005, 280:7206-7217.
62. Piper D.R., Varghese A., Sanguinetti M.C., Tristani-Firouzi M. Gating currents associated with intramembrane charge displacement in HERG potassium channels. Proc. Natl. Acad. Sci. USA 2003, 100:10534-10539.
63. + channel selectively modulates channel gating. Proc. Natl. Acad. Sci. USA. 1995, 92:9422-9426.
64. + channels. Circ. Res. 1998, 82:739-750.
65. + ion channels. J. Biol. Chem. 2010, 285(6):4130-4142.
66. + channels in the central nervous system. Mol. Pharmacol. 2006, 69:1673-1683.
67. + channels, purified from the Mexican scorpion Centruroides elegans elegans. Neurochem. Res. 2008, 33:1525-1533.
68. + channels and scorpion toxins. Trends Pharmacol. Sci. 2003, 24:222-227.
69. + channels. Toxicon 2004, 43:865-875.
70. Rodriguez-de-la-Vega R., Barraza R., Restano R., Possani L.D. Toxins Active on Herg Channel: Structure and Function, en: de Lima M.E. Animal Toxins: State of the Art. Perspectives in Health and Biotechnology. Belo Horizonte 2009, Universidad de Minas Gerais, 193-204.
71. Rosati B., Marchetti P., Crociani O., Lecchi M., Lupi R., Arcangeli A., Olivotto M., Wanke E. Glucose- and arginine-induced insulin secretion by human pancreatic beta-cells: the role of HERG K(+) channels in firing and release. FASEB J. 2000, 14:2601-2610.
72. vAP. Biochemistry 2004, 43:10071-10079.
73. Saganich M.J., Machado E., Rudy B. Differential expression of genes encoding subthreshold-operating voltage-gated K+ channels in brain. J. Neurosci. 2001, 21:4609-4624.
74. Sanguinetti M.C., Jiang C., Curran M.E., Keating M.T. A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel. Cell 1995, 81:299-307.
75. Schönherr R., Heinemann S. Molecular determinants for activation and inactivation of HERG, a human inward rectifier potassium channel. J. Physiol. 1996, 493:635-642.
76. + channel. Neuron 1996, 16:1159-1167.
77. Shi W., Wymore R.S., Wang H.S., Pan Z., Cohen I.S., McKinnon D., Dixon J.E. Identification of two nervous system-specific members of the erg potassium channel gene family. J. Neurosci. 1997, 17:9423-9432.
78. Smith P.L., Baukrowitz T., Yellen G. The inward rectification mechanism of the HERG cardiac potassium channel. Nature 1996, 379:833-836.
79. Smith P.L., Yellen G. Fast and slow voltage sensor movements in HERG potassium channels. J. Gen. Physiol. 2002, 119:275-293.
80. Subbiah R.N., Clarke C.E., Smith D.J., Zhao J.T., Campbell T.J., Vandenberg J.I. Molecular basis of slow activation of the human ether-á-go-go related gene potassium channel. J. Physiol. 2004, 558:417-431.
81. + channel: the S4 domain is loosely packed and likely to be lipid exposed. J. Physiol. 2005, 569:367-379.
82. Suchyna T.M., Tape S.E., Koeppe R.E., Andersen O.S., Sachs F., Gottlieb P.A. Bilayer-dependent inhibition of mechanosensitive channels by neuroactive peptide enantiomers. Nature 2000, 430:235-240.
83. + channels. Neuron 1997, 18:675-682.
84. Thomas D., Kiehn J., Katus H.A., Karle C.A. Defective protein trafficking in hERG-associated hereditary long QT syndrome (LQT2): molecular mechanisms and restoration of intracellular protein processing. Cardio Res. 2003, 60:235-241.
85. + channel S5P extracellular linker: role of an amphipathic alpha-helix in C-type inactivation. J. Biol. Chem. 2003, 278:42136-42148.
86. Tristani-Firouzi M., Sanguinetti M.C. Structural determinants and biophysical properties of HERG and KCNQ1 channel gating. J. Mol. Cellular Cardiol. 2003, 35:27-35.
87. Trudeau M.C., Warmke J.M., Ganetzky B., Robertson G.A. HERG, a human inward rectifier in the voltage-gated potassium channel family. Science 1995, 269:92-95.
88. Tseng G.N., Sonawane K.D., Korolkova Y.V., Zhang M., Liu J., Grishin E.V., Guy R.H. Probing the outer mouth structure of the hERG channel wit peptide toxin footprinting and molecular modeling. Biophys. J. 2007, 92:3524-3540.
89. Tytgat J., Chandy K.G., Garcia L.M., Gutman G.A., Martin-Eauclaire M.F., van del Walt J.J., Possani L.D. A unified nomenclature for short chain peptides isolated from scorpion venoms: alpha-KTx molecular subfamilies. Trends Pharmacol. Sci. 1999, 20:445-447.
90. Vacher H., Alami M., Crest M., Possani L.D., Bougis P.E., Martin-Eauclaire M.F. Expanding the scorpion toxin alpha-KTX15 family with AmmX3 from Androctonus mauritanicus. Eur. J. Biochem. 2001, 269:6037-6040.
91. + channel: pharmacological characterization and localization in rat brain. FEBS Lett. 2002, 501:31-36.
92. Viloria C.G., Barros F., Giraldez T., Gomez-Varela D., de la Pena P. Differential effects of amino-terminal distal and proximal domains in the regulation of human erg K(+) cannel gating. Biophys. J. 2000, 79:231-246.
93. Warmke J.W., Ganeztky B. A family of potassium channel genes related to eag in Drosophila and mammals. Proc. Natl. Acad. Sci. USA 1994, 91(8):3438-3442.
94. Wimmers S., Wuflsen I., Bauer C.K., Schwarz J.R. Erg1, erg2 and erg3 K channel subunits are able to form heteromultimers. Pflueg Arch. Eur. J. Physiol. 2001, 441:450-455.
95. + channel allows inactivation to be modulated by metal binding. Biophys. J. 1994, 66:1068-1075.
96. Zhang M., Korolkova Y.V., Liu J., Jiang M., Grishin E.V., Tseng G.N. BeKm-1 is a HERG-specific toxin that shares the structure with ChTx but the mechanism of action with ErgTx1. Biophys. J. 2003, 84:3022-3036.
97. Zhang M., Liu J., Tseng G.N. Gating charges in the activation and inactivation processes of the hERG channel. J. Gen. Physiol. 2004, 124:703-718.
98. Zhang M., Liu X.S., Diochot S., Lazdunski M., Tseng G.N. APETx1 from sea anemone Antopleura elegantissima is a gating modifier peptide toxin of the human ether-a-go-go-related potassium channel. Mol. Pharmacol. 2007, 72:259-268.