Mechanisms of distribution and targeting of neuronal ion channels

Current Opinion in Drug Discovery and Development

Volumn 13, Issue 5, 2010, Pages 559-567

  Thayer, Desiree A ^a   Jan, Lily Y ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

Fluorescent indicator; high throughput screening; HTS; ion channel; multi target drug; neurotoxin; planar array patch clamp

Indexed keywords

ION CHANNEL; NEUROTOXIN;

DRUG DISTRIBUTION; DRUG MECHANISM; DRUG RESEARCH; DRUG SCREENING; DRUG TARGETING; ELECTROPHYSIOLOGY; HUMAN; NERVE CELL; NONHUMAN; REVIEW;

ANIMALS; CELLS, CULTURED; CENTRAL NERVOUS SYSTEM AGENTS; DRUG DISCOVERY; HUMANS; ION CHANNELS; LIGANDS; MEMBRANE POTENTIALS; NEURONS; NEUROTOXINS; PATCH-CLAMP TECHNIQUES; PROTEIN BINDING; SPECTROPHOTOMETRY, ATOMIC;

EID: 77956409787     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (70)

1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov (2006) 5(12):993-996.
2. Jegla TJ, Zmasek CM, Batalov S, Nayak SK: Evolution of the human ion channel set. Comb Chem High Throughput Screen (2009) 12(1):2-23
3. Carpenter EP, Beis K, Cameron AD, Lwata S: Overcoming the challenges of membrane protein crystallography. Curr Opin Struc Biol (2008) 18(5):581-586.
4. Nilius B, Owsianik G: Transient receptor potential channelopathies. Pflugers Arch (2010) 460(2):437-450.
5. Vriens J, Appendino G, Nilius B: Pharmacology of vanilloid transient receptor potential cation channels. Mol Pharmacol (2009) 75(6):1262-1279.
6. Calixto JB, Kassuya CAL, André E, Ferreira J: Contribution of natural products to the discovery of the transient receptor potential (TRP) channels family and their functions. Pharmacol Ther (2005) 106(2):179-208.
7. Appendino G, Minassi A, Pagani A, Ech-Chahad A: The role of natural products in the ligand deorphanization of TRP channels. Curr Pharm Des (2008) 14(1):2-17.
8. Clare JJ, Chen MX, Downie DL, Trezise DJ, Powell AJ: Use of planar array electrophysiology for the development of robust ion channel cell lines. Comb Chem High Throughput Screen (2009) 12(1):96-106.
9. Bianchi BR, Moreland RB, Faltynek CR, Chen J: Application of large-scale transiently transfected cells to functional assays of ion channels: Different targets and assay formats. Assay Drug Dev Technol (2007) 5(3):417-424.
10. Nekrasova OV, Ignatova AA, Nazarova AI, Feofanov AV, Korolkova YV, Boldyreva EF, Tagvei AI, Grishin EV, Arseniev AS, Kirpichnikov MP: Recombinant Kv channels at the membrane of Escherichia coli bind specifically agitoxin2. J Neuroimmune Pharmacol (2009) 4(1):83-91.
11. Poulos JL, Jeon T, Damoiseaux R, Gillespie EJ, Bradley KA, Schmidt JJ: Ion channel and toxin measurement using a high throughput lipid membrane platform. Biosens Bioelectron (2009) 24(6):1806-1810.
12. Suzuki H, Le Pioufle B, Takeuchi S: Ninety-six-well planar lipid bilayer chip for ion channel recording fabricated by hybrid stereolithography. Biomed Microdevices (2009) 11(1):17-22.
13. Triggle DJ, Gopalakrishnan M, Rampe D, Zheng W (Eds): Voltage-gated ion channels as drug targets. John Wiley and Sons, Hoboken, NJ, USA (2006).
14. Joesch C, Guevarra E, Parel SP, Bergner A, Zbinden P, Konrad D, Albrecht H: Use of FLIPR membrane potential dyes for validation of high-throughput screening with the FLIPR and microARCS technologies: Identification of ion channel modulators acting on the GABAA receptor. J Biomol Screen (2008) 13(3):218-228.
15. Shoshan-Barmatz V, Israelson A, Brdiczka D, Sheu SS: The voltage-dependent anion channel (VDAC): Function in intracellular signalling, cell life and cell death. Curr Pharm Des (2006) 12(18):2249-2270.
16. Slack M, Kirchhoff C, Moller C, Winkler D, Netzer R: Identification of novel kv1.3 blockers using a fluorescent cell-based ion channel assay. J Biomol Screen (2006) 11(1):57-64.
17. Solly K, Cassaday J, Felix JP, Garcia ML, Ferrer M, Strulovici B, Kiss L: Miniaturization and HTS of a FRET-based membrane potential assay for Kir channel inhibitors. Assay Drug Dev Technol (2008) 6(2):225-234.
18. Trivedi S, Dekermendjian K, Julien R, Huang J, Lund PE, Krupp J, Kronqvist R, Larsson O, Bostwick R: Cellular HTS assays for pharmacological characterization of NaV1.7 modulators. Assay Drug Dev Technol (2008) 6(2):167-179.
19. Tang Y, Li X, He J, Lu J, Diwu Z: Real-time and high throughput monitoring of cAMP in live cells using a fluorescent membrane potential-sensitive dye. Assay Drug Dev Technol (2006) 4(4):461-471.
20. Dai G, Haedo RJ, Warren VA, Ratliff KS, Bugianesi RM, Rush A, Williams ME, Herrington J, Smith MM, McManus OB, Swensen AM: A high-throughput assay for evaluating state dependence and subtype selectivity of Cav2 calcium channel inhibitors. Assay Drug Dev Technol (2008) 6(2):195-212.
21. Weaver CD, Harden D, Dworetzky SI, Robertson B, Knox RJ: A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells. J Biomol Screen (2004) 9(8):671-677.
22. Hille B: The permeability of the sodium channel to metal cations in myelinated nerve. J Gen Physiol (1972) 59(6): 637-658.
23. Graefe A, Stanca SE, Nietzsche S, Kubicova L, Beckert R, Biskup C, Mohr GJ: Development and critical evaluation of fluorescent chloride nanosensors. Anal Chem (2008) 80(17):6526-6531.
24. Menon V, Ranganathn A, Jorgensen V, Sabio M, Christoffersen C, Uberti M, Jones K, Babu P: Development of an aequorin luminescence calcium assay for high-throughput screening using a plate reader, the lumilux. Assay Drug Dev Technol (2008) 6(6):787-793.
25. Walstab J, Combrink S, Brss M, Göthert M, Niesler B, Bönisch H: Aequorin luminescence-based assay for 5-hydroxytryptamine (serotonin) type 3 receptor characterization. Anal Biochem (2007) 368(2):185-192.
26. Bovolenta S, Foti M, Lohmer S, Corazza S: Development of a Ca2+-activated photoprotein, photina, and its application to high-throughput screening. J Biomol Screen (2007) 12(5): 694-704.
27. Vasilyev D, Merrill T, Iwanow A, Dunlop J, Bowlby M: A novel method for patch-clamp automation. Pflugers Arch (2006) 452(2):240-247.
28. Fejtl M, Czubayko U, Hummer A, Krauter T, Lepple-Wienhues A: Flip-the-tip: Automated patch clamping based on glass electrodes. Methods Mol Biol (2007) 403:71-85.
29. Papke RL, Smith-Maxwell C: High throughput electrophysiology with Xenopus oocytes. Comb Chem High Throughput Screen (2009) 12(1):38-50.
30. Dunlop J, Bowlby M, Peri R, Vasilyev D, Arias R: High-throughput electrophysiology: An emerging paradigm for ion-channel screening and physiology. Nat Rev Drug Discov (2008) 7(4): 358-368.
31. Ratliff KS, Petrov A, Eiermann GJ, Deng Q, Green MD, Kaczorowski GJ, McManus OB, Herrington J: An automated electrophysiology serum shift assay for KV channels. Assay Drug Dev Technol (2008) 6(2):243-253.
32. John VH, Dale TJ, Hollands EC, Chen MX, Partington L, Downie DL, Meadows HJ, Trezise DJ: Novel 384-well population patch clamp electrophysiology assays for Ca2+-activated K+ channels. J Biomol Screen (2007) 12(1):50-60.
33. Castle N, Printzenhoff D, Zellmer S, Antonio B, Wickenden A, Silvia C: Sodium channel inhibitor drug discovery using automated high throughput electrophysiology platforms. Comb Chem High Throughput Screen (2009) 12(1):107-122.
34. Korsgaard MPG, Strobaek D, Christophersen P: Automated planar electrode electrophysiology in drug discovery: Examples of the use of QPatch in basic characterization and high content screening on Nav, KCa2.3, and Kv11.1 channels. Comb Chem High Throughput Screen (2009) 12(1):51-63.
35. Schrder RL, Friis S, Sunesen M, Mathes C, Willumsen NJ: Automated patch-clamp technique: increased throughput in functional characterization and in pharmacological screening of small-conductance Ca2+ release-activated Ca2+ channels. J Biomol Screen (2008) 13(7):638-647.
36. Mathes C, Friis S, Finley M, Liu Y: QPatch: The missing link between HTS and ion channel drug discovery. Comb Chem High Throughput Screen (2009) 12(1):78-95.
37. Beck EJ, Hutchinson TL, Qin N, Flores CM, Liu Y: Development and validation of a secondary screening assay for TRPM8 antagonists using QPatch HT. Assay Drug Dev Technol (2010) 8(1):63-72.
38. Farre C, Haythornthwaite A, Haarmann C, Stoelzle S, Kreir M, George M, Brueggemann A, Fertig N: Port-a-patch and patchliner: High fidelity electrophysiology for secondary screening and safety pharmacology. Comb Chem High Throughput Screen (2009) 12(1):24-37.
39. Dahan E, Bize V, Lehnert T, Horisberger JD, Gijs MA: Rapid fluidic exchange microsystem for recording of fast ion channel kinetics in xenopus oocytes. Lab Chip (2008) 8(11): 1809-1818.
40. Botzolakis EJ, Maheshwari A, Feng HJ, Lagrange AH, Shaver JH, Kassebaum NJ, Venkataraman R, Baudenbacher F, Macdonald RL: Achieving synaptically relevant pulses of neurotransmitter using PDMS microfluidics. J Neurosci Methods (2009) 177(2): 294-302.
41. Lepple-Wienhues A, Lassen D, Huemmer A, Czubayko U, Knirsch M, Golubovic A: The chiptip: A novel tool for automated patch clamp. Comb Chem High Throughput Screen (2009) 12(1):73-77
42. Bingham J-P, Mitsunaga E, Bergeron ZL: Drugs from slugs - Past, present and future perspectives of omega-conotoxin research. Chem-Biol Interact (2010) 183(1):1-18.
43. Escoubas P, Quinton L, Nicholson GM: Venomics: Unravelling the complexity of animal venoms with mass spectrometry. J Mass Spectrom (2008) 43(3):279-295.
44. Olivera BM: Conus peptides: Biodiversity-based discovery and exogenomics. J Biol Chem (2006) 281(42):31173-31177.
45. Bulaj G, West PJ, Garrett JE, Watkins M, Marsh M, Zhang MM, Norton RS, Smith BJ, Yoshikami D, Olivera BM: Novel conotoxins from Conus striatus and Conus kinoshitai selectively block TTX-resistant sodium channels. Biochemistry (2005) 44(19): 7259-7265.
46. Ellison M, Feng ZP, Park AJ, Zhang X, Olivera BM, McIntosh JM, Norton RS: α-RgIA, a novel conotoxin that blocks the α9α10 nAChR: Structure and identification of key receptorbinding residues. J Mol Biol (2008) 377(4):1216-1227.
47. Holford M, Zhang MM, Gowd KH, Azam L, Green BR, Watkins M, Ownby JP, Yoshikami D, Bulaj G, Olivera BM: Pruning nature: Biodiversity-derived discovery of novel sodium channel blocking conotoxins from Conus bullatus. Toxicon (2009) 53(1):90-98.
48. Twede VD, Miljanich G, Olivera BM, Bulaj G: Neuroprotective and cardioprotective conopeptides: An emerging class of drug leads. Curr Opin Drug Discov Devel (2009) 12(2):231-239.
49. Twede VD, Teichert RW, Walker CS, Gruszczy?ski P, Ka?mierkiewicz R, Bulaj G, Olivera BM: Conantokin-Br from Conus brettinghami and selectivity determinants for the NR2D subunit of the NMDA receptor. Biochemistry (2009) 48(19):4063-4073.
50. University of Utah/Cognetix Inc (Bulaj G OB, Buczek O, Garrett JE, Goodsell I): Nucleic acid sequences encoding conus protein disulfide isomerase. US-07238513 (2007).
51. Zhou X, Sun Q, Kini RM, Sivaraman J: A universal method for fishing target proteins from mixtures of biomolecules using isothermal titration calorimetry. Protein Sci (2008) 17(10): 1798-1804.
52. Legros C, Guette C, Martin-Eauclaire M, Goyffon M, Tortajada J: Affinity capture using chimeric membrane proteins bound to magnetic beads for rapid ligand screening by matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. Rapid Commun Mass Spectrom (2009) 23(6):745-755.
53. Han TS, Zhang MM, Walewska A, Gruszczynski P, Robertson CR, Cheatham TE, Yoshikami D, Olivera BM, Bulaj G: Structurally minimized mu-conotoxin analogues as sodium channel blockers: Implications for designing conopeptide-based therapeutics. ChemMedChem (2009) 4(3):406-414.
54. Darlak K, Wiegandt Long D, Czerwinski A, Darlak M, Valenzuela F, Spatola AF, Barany G: Facile preparation of disulfide-bridged peptides using the polymer-supported oxidant CLEAR-OX. J Pept Res (2004) 63(3):303-312.
55. Green BR, Bulaj G: Oxidative folding of conotoxins in immobilized systems. Protein Pept Lett (2006) 13(1):67-70.
56. Buczek O, Green BR, Bulaj G: Albumin is a redox-active crowding agent that promotes oxidative folding of cysteinerich peptides. Biopolymers (2007) 88(1):8-19.
57. Altamirano MM, García C, Possani LD, Fersht AR: Oxidative refolding chromatography: Folding of the scorpion toxin Cn5. Nat Biotechnol (1999) 17(2):187-191.
58. Armishaw CJ, Daly NL, Nevin ST, Adams DJ, Craik DJ, Alewood PF: α-Selenoconotoxins, a new class of potent α7 neuronal nicotinic receptor antagonists. J Biol Chem (2006) 281(20):14136-14143.
59. Bondebjerg J, Grunnet M, Jespersen T, Meldal M: Solid-phase synthesis and biological activity of a thioether analogue of conotoxin G1. Chembiochem (2003) 4(2-3):186-194.
60. Robinson AJ, Elaridi J, Van Lierop BJ, Mujcinovic S, Jackson WR: Microwave-assisted RCM for the synthesis of carbocyclic peptides. J Pept Sci (2007) 13(4):280-285.
61. Derksen DJ, Stymiest JL, Vederas JC: Antimicrobial leucocin analogues with a disulfide bridge replaced by a carbocycle or by noncovalent interactions of allyl glycine residues. J Am Chem Soc (2006) 128(44):14252-14253.
62. Gottler LM, de la Salud-Bea R, Marsh EN: The fluorous effect in proteins: Properties of α4F6, a 4-α-helix bundle protein with a fluorocarbon core. Biochemistry (2008) 47(15): 4484-4490.
63. Green BR, Catlin P, Zhang MM, Fiedler B, Bayudan W, Morrison A, Norton RS, Smith BJ, Yoshikami D, Olivera BM, Bulaj G: Conotoxins containing nonnatural backbone spacers: Cladistic-based design, chemical synthesis, and improved analgesic activity. Chem Biol (2007) 14(4):399-407.
64. Blanchfield JT, Dutton JL, Hogg RC, Gallagher OP, Craik DJ, Jones A, Adams DJ, Lewis RJ, Alewood PF, Toth I: Synthesis, structure elucidation, in vitro biological activity, toxicity, and Caco-2 cell permeability of lipophilic analogues of α-conotoxin MII. J Med Chem (2003) 46(7):1266-1272.
65. Roth BL, Sheffler DJ, Kroeze WK: Magic shotguns versus magic bullets: Selectively non-selective drugs for mood disorders and schizophrenia. Nat Rev Drug Discov (2004) 3(4):353-359.
66. Bianchi MT, Pathmanathan J, Cash SS: From ion channels to complex networks: Magic bullet versus magic shotgun approaches to anticonvulsant pharmacotherapy. Med Hypotheses (2009) 72(3):297-305.
67. Bianchi MT: Promiscuous modulation of ion channels by anti-psychotic and anti-dementia medications. Med Hypotheses (2010) 74(2):297-300.
68. Prisinzano TE: Natural products as tools for neuroscience: Discovery and development of novel agents to treat drug abuse. J Nat Prod (2009) 72(3):581-587.
69. McCurdy CR, Scully SS: Analgesic substances derived from natural products (natureceuticals). Life Sci (2005) 78(5): 476-484.
70. Stett A, Burkhardt C, Weber U, van Stiphout P, Knott T: CYTOCENTERING: A novel technique enabling automated cell-by-cell patch clamping with the CYTOPATCH chip. Receptors Channels (2003) 9(1):59-66.