A high-throughput assay for evaluating state dependence and subtype selectivity of Cav2 calcium channel inhibitors

Assay and Drug Development Technologies

Volumn 6, Issue 2, 2008, Pages 195-212

  Dai, Ge ^a   Haedo, Rodolfo J ^a   Warren, Vivien A ^a   Ratliff, Kevin S ^a   Bugianesi, Randal M ^a   Rush, Alison ^a   Williams, Mark E ^a,b   Herrington, James ^a   Smith, McHardy M ^a   McManus, Owen B ^a   Swensen, Andrew M ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b Senomyx Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CALCIUM CHANNEL BLOCKING AGENT; CALCIUM CHANNEL CAV2.1; CALCIUM CHANNEL CAV2.2; CALCIUM CHANNEL CAV2.3; INWARDLY RECTIFYING POTASSIUM CHANNEL; INWARDLY RECTIFYING POTASSIUM CHANNEL SUBUNIT KIR2.3; OMEGA CONOTOXIN MVIIA; VOLTAGE GATED CALCIUM CHANNEL;

ARTICLE; CALCIUM CURRENT; CALCIUM TRANSPORT; CONTROLLED STUDY; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; MEMBRANE POTENTIAL; NUCLEOTIDE SEQUENCE;

BLOTTING, WESTERN; CALCIUM; CALCIUM CHANNEL BLOCKERS; CAVEOLIN 2; CELL LINE; DRUG EVALUATION, PRECLINICAL; ELECTROPHYSIOLOGY; HUMANS; IMMUNOHISTOCHEMISTRY; MEMBRANE POTENTIALS; PATCH-CLAMP TECHNIQUES; POTASSIUM; POTASSIUM CHANNELS, INWARDLY RECTIFYING; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION;

EID: 43449137258     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2008.136     Document Type: Article

References (56)

1. Luebke JI, Dunlap K, Turner TJ: Multiple calcium channel types control glutamatergic synaptic transmission in the hippocampus. Neuron 1993;11:895-902.
2. Mintz IM, Sabatini BL, Regehr WG: Calcium control of transmitter release at a cerebellar synapse. Neuron 1995;15:675-688.
3. 2+ channels mediate transmitter release with a similar cooperativity at rat hippocampal autapses. J Neurosci 1998;18:2849-2855.
4. 2+ channels: a functional patchwork. Trends Neurosci 2003;26:683-687.
5. 2+ channels in supporting hippocampal synaptic transmission. Science 1994;264:107-111.
6. 1A-subunit. Proc Natl Acad Sci U S A 1999;96:15245-15250.
7. Pietrobon D: Function and dysfunction of synaptic calcium channels: insights from mouse models. Curr Opin Neurobiol 2005;15:257-265.
8. V2.1 in absence epilepsy and episodic ataxia. Brain 2004;127:2682-2692.
9. 2+ channel gene CACNL1A4. Cell 1996;87:543-552.
10. 2+ channels. Neuroreport 2001;12:2423-2427.
11. 1B subunit of the voltage-dependent calcium channel. Mol Cell Neurosci 2001;18:235-245.
12. 2+ channel. EMBO J 2001;20:2349-2356.
13. Staats PS, Yearwood T, Charapata SG, Presley RW, Wallace MS, Byas-Smith M, et al.: Intrathecal ziconotide in the treatment of refractory pain in patients with cancer or AIDS - a randomized controlled trial. JAMA 2004;291:63-70.
14. Wallace MS, Charapata SG, Fisher R, Byas-Smith M, Staats PS, Mayo M, et al.: Intrathecal ziconotide in the treatment of chronic nonmalignant pain: a randomized, double-blind, placebo-controlled clinical trial. Neuromodulation 2006;9:75-86.
15. Wermeling DR: Ziconotide, an intrathecally administered N-type calcium channel antagonist for the treatment of chronic pain. Pharmacotherapy 2005;25:1084-1094.
16. 2+ channel. Proc Natl Acad Sci U S A 2000;97:6132-6137.
17. Wilson SM, Toth PT, Oh SB, Gillard SE, Volsen S, Ren D, et al.: The status of voltage-dependent calcium channels in alpha 1E knock-out mice. J Neurosci 2000;20:8566-8571.
18. Matthews EA, Bee LA, Stephens GJ, Dickenson AH: The Cav2.3 calcium channel antagonist SNX-482 reduces dorsal horn neuronal responses in a rat model of chronic neuropathic pain. Eur J Neurosci 2007;25:3561-3569.
19. Murakami M, Nakagawasai O, Suzuki T, Mobarakeh II, Sakurada Y, Murata A, et al.: Antinociceptive effect of different types of calcium channel inhibitors and the distribution of various calcium channel alpha 1 subunits in the dorsal horn of spinal cord in mice. Brain Res 2004;1024:122-129.
20. McGivern JG, McDonough SI: Voltage-gated calcium channels as targets for the treatment of chronic pain. Curr Drug Targets CNS Neurol Disord 2004;3:457-478.
21. Snutch TP: Targeting chronic and neuropathic pain: the Ntype calcium channel comes of age. NeuroRx 2005;2:662-670.
22. v2.2 voltage-gated calcium channels for neuropathic pain. Biochem Pharmacol 2005;70:489-499.
23. Hamill OP, Marty A, Neher E, Sakmann B, Sigworth FJ: Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflugers Arch 1981;391:85-100.
24. Xia MH, Imredy JP, Koblan KS, Bennett P, Connolly TM: State-dependent inhibition of L-type calcium channels: cell-based assay in high-throughput format. Anal Biochem 2004;327:74-81.
25. v3 T-type channels using molecular and pharmacologic approaches. Assay Drug Dev Technol 2007;5:191-203.
26. Bleakman D, Bowman D, Bath CP, Brust PF, Johnson EC, Deal CR, et al.: Characteristics of a human N-type calcium-channel expressed in HEK293 cells. Neuropharmacology 1995;34:753-765.
27. Hans M, Urrutia A, Deal C, Brust PF, Stauderman K, Ellis SB, et al.: Structural elements in domain IV that influence biophysical and pharmacological properties of human alpha1A-containing high-voltage-activated calcium channels. Biophys J 1999;76:1384-1400.
28. Williams ME, Brust PF, Feldman DH, Patthi S, Simerson S, Maroufi A, et al.: Structure and functional expression of an omega-conotoxin sensitive human N-type calcium-channel. Science 1992;257:389-395.
29. 1E calcium-channel subtypes. J Biol Chem 1994;269:22347-22357.
30. Williams ME, Feldman DH, McCue AF, Brenner R, Velicelebi G, Ellis SB, et al.: Structure and functional expression of alpha-1-subunit, alpha-2-subunit, and beta-subunit of a novel human neuronal calcium-channel subtype. Neuron 1992;8:71-84.
31. Harpold MM, Ellis SB, Williams ME, McCue AF: Human calcium channel compositions and methods. US Patent 6,096,514. August 1, 2000.
32. Perier F, Radeke CM, Vandenberg CA: Primary structure and characterization of a small-conductance inwardly rectifying potassium channel from human hippocampus. Proc Natl Acad Sci U S A 1994;91:6240-6244.
33. Beattie RE, Volsen SG, Smith D, McCormack AL, Gillard SE, Burnett JP, et al.: Preparation and purification of antibodies specific to human neuronal voltage-dependent calcium channel subunits. Brain Res Brain Res Protoc 1997;1:307-319.
34. Canti C, Davies A, Berrow NS, Butcher AJ, Page KM, Dolphin AC: Evidence for two concentration-dependent processes for beta-subunit effects on alpha 1B calcium channels. Biophys J 2001;81:1439-1451.
35. 1 subunits at the human and rat neuromuscular junction. J Neurosci 1997;17:6226-6235.
36. Feigenbaum P, Garcia ML, Kaczorowski GJ: Evidence for distinct sites coupled to high-affinity omega-conotoxin receptors in rat-brain synaptic plasma-membrane vesicles. Biochem Biophys Res Commun 1988;154:298-305.
37. Neher E: Correction for liquid junction potentials in patch clamp experiments. Methods Enzymol 1992;207:123-131.
38. Mintz IM, Venema VJ, Swiderek KM, Lee TD, Bean BP, Adams ME: P-type calcium channels blocked by the spider toxin omega-Aga-IVA. Nature 1992;355:827-829.
39. Olivera BM, Gray WR, Zeikus R, McIntosh JM, Varga J, Rivier J, et al.: Peptide neurotoxins from fish-hunting cone snails. Science 1985;230:1338-1343.
40. Reynolds IJ, Wagner JA, Snyder SH, Thayer SA, Olivera BM, Miller RJ: Brain voltage-sensitive calcium-channel subtypes differentiated by omega-conotoxin fraction GVIA. Proc Natl Acad Sci U S A 1986;83:8804-8807.
41. Newcomb R, Szoke B, Palma A, Wang G, Chen X, Hopkins W, et al.: Selective peptide antagonist of the class E calcium channel from the venom of the tarantula Hysterocrates gigas. Biochemistry 1998;37:15353-15362.
42. Hille B, Woodhull AM, Shapiro BI: Negative surface charge near sodium channels of nerve: divalent ions, monovalent ions, and pH. Philos Trans R Soc Lond B Biol Sci 1975;270:301-318.
43. V2.3) calcium channels. Biophys J 2001;81:79-88.
44. McDonough SI, Boland LM, Mintz IM, Bean BP: Interactions among toxins that inhibit N-type and P-type calcium channels. J Gen Physiol 2002;119:313-328.
45. McDonough SI, Mintz IM, Bean BP: Alteration of P-type calcium channel gating by the spider toxin omega-Aga-IVA. Biophys J 1997;72:2117-2128.
46. v2.2) mediated calcium mobilization using FLIPR. Biochem Pharmacol 2006;72:770-782.
47. Lubin ML, Reitz TL, Todd MJ, Flores CM, Qin N, Xin H: A nonadherent cell-based HTS assay for N-type calcium channel using calcium 3 dye. Assay Drug Dev Technol 2006;4:689-694.
48. 2+ channels. Eur J Pharm Sci 2002;15:321-330.
49. Zhang SP, Kauffman J, Yagel SK, Codd EE: High-throughput screening for N-type calcium channel blockers using a scintillation proximity assay. J Biomol Screen 2006;11:672-677.
50. 1A subunit gene generates phenotypic variants of P- and Q-type calcium channels. Nat Neurosci 1999;2:407-415.
51. 2delta subunits of voltage-gated calcium channels. Trends Pharmacol Sci 2007;28:220-228.
52. +2 channels. Nat Neurosci 2007;10:691-701.
53. v2.2 channels by 14-3-3 proteins. Neuron 2006;51:755-771.
54. 1-subunit. Nature 1994;368:67-70.
55. Patil PG, Brody DL, Yue DT: Preferential closed-state inactivation of neuronal calcium channels. Neuron 1998;20:1027-1038.
56. McDonough SI, Swartz KJ, Mintz IM, Boland LM, Bean BP: Inhibition of calcium channels in rat central and peripheral neurons by omega-conotoxin MVIIC. J Neurosci 1996;16:2612-2623.