Targeting the voltage sensor of Kv7.2 voltage-gated K+ channels with a new gating-modifier

Proceedings of the National Academy of Sciences of the United States of America

Volumn 107, Issue 35, 2010, Pages 15637-15642

  Peretz, Asher ^a   Pell, Liat ^a   Gofman, Yana ^a   Haitin, Yoni ^a   Shamgar, Liora ^a   Patrich, Eti ^a   Kornilov, Polina ^a   Gourgy Hacohen, Orit ^a   Ben Tal, Nir ^a   Attali, Bernard ^a  

^a TEL AVIV UNIVERSITY   (Israel)

Author keywords

Ion channel; KCNQ; M current; Opener

Indexed keywords

4 AMINOBUTYRIC ACID; GLUTAMIC ACID; NH29; POTASSIUM CHANNEL KV7.2; POTASSIUM CHANNEL STIMULATING AGENT; RETIGABINE; SCORPION VENOM; SEA ANEMONE TOXIN; SPIDER VENOM; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1; VOLTAGE GATED POTASSIUM CHANNEL;

4 AMINOBUTYRIC ACID RELEASE; ANIMAL CELL; ARTICLE; CHANNEL GATING; ELECTRIC POTENTIAL; EXCITATORY POSTSYNAPTIC POTENTIAL; HIPPOCAMPUS; INHIBITORY POSTSYNAPTIC POTENTIAL; MUTAGENESIS; NERVE CELL; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; ANTHRANILIC ACIDS; BINDING SITES; CALCIUM CHANNEL BLOCKERS; CHO CELLS; CRICETINAE; CRICETULUS; EXCITATORY POSTSYNAPTIC POTENTIALS; HUMANS; INHIBITORY POSTSYNAPTIC POTENTIALS; ION CHANNEL GATING; KCNQ2 POTASSIUM CHANNEL; KINETICS; MEMBRANE POTENTIALS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; MUTATION; NEURONS; NEUROTRANSMITTER AGENTS; PROTEIN MULTIMERIZATION; PROTEIN STRUCTURE, TERTIARY; TRANSFECTION; TRPV CATION CHANNELS;

ACTINIARIA; SCORPIONES; TARANTULA;

EID: 77957276699     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.0911294107     Document Type: Article

References (37)

1. Ashcroft FM (2000) Ion Channels and Diseases (Academic Press, Oxford).
2. Camerino DC, Tricarico D, Desaphy JF (2007) Ion channel pharmacology. Neurotherapeutics 4(2):184-198.
3. Swartz KJ (2008) Sensing voltage across lipid membranes. Nature 456:891-897.
4. Murata Y, Iwasaki H, Sasaki M, Inaba K, Okamura Y (2005) Phosphoinositide phosphatase activity coupled to an intrinsic voltage sensor. Nature 435:1239-1243. (Pubitemid 40943089)
5. Ramsey IS, Moran MM, Chong JA, Clapham DE (2006) A voltage-gated proton-selective channel lacking the pore domain. Nature 440:1213-1216.
6. Sasaki M, Takagi M, Okamura Y (2006) A voltage sensor-domain protein is a voltage-gated proton channel. Science 312:589-592.
7. Lee SY, Letts JA, MacKinnon R (2009) Functional reconstitution of purified human Hv1 H+ channels. J Mol Biol 387:1055-1060.
8. Jiang Y, et al. (2003) X-ray structure of a voltage-dependent K+ channel. Nature 423: 33-41.
9. Long SB, Campbell EB, Mackinnon R (2005) Crystal structure of a mammalian voltage-dependent Shaker family K+ channel. Science 309:897-903.
10. Alabi AA, Bahamonde MI, Jung HJ, Kim JI, Swartz KJ (2007) Portability of paddle motif function and pharmacology in voltage sensors. Nature 450:370-375.
11. Peretz A, et al. (2007) A tale of switched functions: From cyclooxygenase inhibition to M-channel modulation in new diphenylamine derivatives. PLoS ONE 2:e1332.
12. Delmas P, Brown DA (2005) Pathways modulating neural KCNQ/M (Kv7) potassium channels. Nat Rev Neurosci 6:850-862.
13. Jentsch TJ (2000) Neuronal KCNQ potassium channels: Physiology and role in diseases. Nat Rev Neurosci 1:21-30.
14. Siemens J, et al. (2006) Spider toxins activate the capsaicin receptor to produce inflammatory pain. Nature 444:208-212.
15. Swartz KJ (2007) Tarantula toxins interacting with voltage sensors in potassium channels. Toxicon 49:213-230.
16. Catterall WA, et al. (2007) Voltage-gated ion channels and gating modifier toxins. Toxicon 49(2):124-141. (Pubitemid 46151715)
17. Peretz A, et al. (2007) Pre- and postsynaptic activation of M-channels by a novel opener dampens neuronal firing and transmitter release. J Neurophysiol 97:283-295.
18. Peretz A, et al. (2005) Meclofenamic acid and diclofenac, novel templates of KCNQ2/Q3 potassium channel openers, depress cortical neuron activity and exhibit anticonvulsant properties. Mol Pharmacol 67:1053-1066.
19. Lange W, et al. (2009) Refinement of the binding site and mode of action of the anticonvulsant Retigabine on KCNQ K+ channels. Mol Pharmacol 75:272-280.
20. Schenzer A, et al. (2005) Molecular determinants of KCNQ (Kv7) K+ channel sensitivity to the anticonvulsant retigabine. J Neurosci 25:5051-5060. (Pubitemid 40712849)
21. Wuttke TV, Seebohm G, Bail S, Maljevic S, Lerche H (2005) The new anticonvulsant retigabine favors voltage-dependent opening of the Kv7.2 (KCNQ2) channel by binding to its activation gate. Mol Pharmacol 67:1009-1017.
22. Dedek K, et al. (2001) Myokymia and neonatal epilepsy caused by a mutation in the voltage sensor of the KCNQ2 K+ channel. Proc Natl Acad Sci USA 98:12272-12277.
23. Xiong Q, Sun H, Li M (2007) Zinc pyrithione-mediated activation of voltage-gated KCNQ potassium channels rescues epileptogenic mutants. Nat Chem Biol 3:287-296. (Pubitemid 46625833)
24. Miceli F, et al. (2008) Gating consequences of charge neutralization of arginine residues in the S4 segment of K(v)7.2, an epilepsy-linked K+ channel subunit. Biophys J 95:2254-2264.
25. Venkatachalam CM, Jiang X, Oldfield T, Waldman M (2003) LigandFit: A novel method for the shape-directed rapid docking of ligands to protein active sites. J Mol Graph Model 21:289-307.
26. Johnson DM, et al. (2006) Functional mapping of the transient receptor potential vanilloid 1 intracellular binding site. Mol Pharmacol 70:1005-1012.
27. Padilla K, Wickenden AD, Gerlach AC, McCormack K (2009) The KCNQ2/3 selective channel opener ICA-27243 binds to a novel voltage-sensor domain site. Neurosci Lett 465(2):138-142.
28. Tiwari-Woodruff SK, Lin MA, Schulteis CT, Papazian DM (2000) Voltage-dependent structural interactions in the Shaker K(+) channel. J Gen Physiol 115(2):123-138.
29. Long SB, Tao X, Campbell EB, MacKinnon R (2007) Atomic structure of a voltage-dependent K+ channel in a lipid membrane-like environment. Nature 450:376-382. (Pubitemid 350126743)
30. Smith JA, Vanoye CG, George AL, Jr, Meiler J, Sanders CR (2007) Structural models for the KCNQ1 voltage-gated potassium channel. Biochemistry 46:14141-14152.
31. Goldenberg O, Erez E, Nimrod G, Ben-Tal N (2009) The ConSurf-DB: Pre-calculated evolutionary conservation profiles of protein structures. Nucleic Acids Res 37 (Database issue):D323-D327.
32. Katoh K, Kuma K, Toh H, Miyata T (2005) MAFFT version 5: Improvement in accuracy of multiple sequence alignment. Nucleic Acids Res 33:511-518.
33. Petrey D, et al. (2003) Using multiple structure alignments, fast model building, and energetic analysis in fold recognition and homology modeling. Proteins 53(Suppl 6): 430-435.
34. Jacobson MP, Friesner RA, Xiang Z, Honig B (2002) On the role of the crystal environment in determining protein side-chain conformations. J Mol Biol 320:597-608. (Pubitemid 34753983)
35. Mayo SL, Olafson BD, Goddard WA (1990) Dreiding: A generic force-field for molecular simulations. J Phys Chem 94:8897-8909.
36. Krammer A, Kirchhoff PD, Jiang X, Venkatachalam CM, Waldman M (2005) LigScore: A novel scoring function for predicting binding affinities. J Mol Graph Model 23:395-407.
37. Muegge I (2006) PMF scoring revisited. J Med Chem 49:5895-5902.