Establishment of a secondary screening assay for P/Q-type calcium channel blockers

Combinatorial Chemistry and High Throughput Screening

Volumn 16, Issue 3, 2013, Pages 233-243

  Hermann, David ^a   Mezler, Mario ^a   Swensen, Andrew M ^b   Bruehl, Claus ^c   Obergrußberger, Ali ^d   Wicke, Karsten ^a   Schoemaker, Hans ^a   Gross, Gerhard ^a   Draguhn, Andreas ^c   Nimmrich, Volker ^a  

^a ABBOTT GMBH AND CO KG   (Germany)

^b ABBOTT LABORATORIES   (United States)

^c UNIVERSITY OF HEIDELBERG   (Germany)

^d NANION TECHNOLOGIES GMBH   (Germany)

Author keywords

Automated patch clamp; Electrophysiology; Ion channel inactivation; Manual patch clamp; P Q type voltage gated calcium channel; Screening protocol; State dependency

Indexed keywords

CALCIUM CHANNEL P TYPE; CALCIUM CHANNEL Q TYPE;

ARTICLE; CONTROLLED STUDY; DEPOLARIZATION; ELECTROPHYSIOLOGY; HUMAN; HUMAN CELL; KINETICS; PATCH CLAMP; PRIORITY JOURNAL; SCREENING;

CALCIUM CHANNEL BLOCKERS; CALCIUM CHANNELS, P-TYPE; CALCIUM CHANNELS, Q-TYPE; CELL LINE; DRUG EVALUATION, PRECLINICAL; HUMANS; PATCH-CLAMP TECHNIQUES; RECOMBINANT PROTEINS;

EID: 84877946399     PISSN: 13862073     EISSN: 18755402     Source Type: Journal    
DOI: 10.2174/1386207311316030008     Document Type: Article

References (44)

1. Imming, P.; Sinning, C.; Meyer, A. Drugs, their targets and the nature and number of drug targets. Nat. Rev. Drug. Discov., 2006, 5(10), 821-834.
2. Catterall, W.A.; Perez-Reyes, E.; Snutch, T.P.; Striessnig, J. International Union of Pharmacology. XLVIII. Nomenclature and structure-function relationships of voltage-gated calcium channels. Pharmacol. Rev., 2005, 57(4), 411-425.
3. Westenbroek, R.E.; Hell, J.W.; Warner, C.; Dubel, S.J.; Snutch, T.P.; Catterall, W.A. Biochemical properties and subcellular distribution of an N-type calcium channel α1 subunit. Neuron, 1992, 9(6), 1099-1115.
4. Rettig, J.; Sheng, Z.H.; Kim, D.K.; Hodson, C.D.; Snutch, T.P.; Catterall, W.A. Isoform-specific interaction of the alpha1A subunits of brain Ca2+ channels with the presynaptic proteins syntaxin and SNAP-25. Proc. Natl. Acad. Sci. U S A, 1996, 93(14), 7363-7368.
5. Reid, C.A.; Bekkers, J.M.; Clements, J.D. Presynaptic Ca2+ channels: a functional patchwork. Trends Neurosci., 2003, 26(12), 683-687.
6. Kerr, L.M.; Yoshikami, D. A venom peptide with a novel presynaptic blocking action. Nature, 1984, 308(5956), 282-284.
7. Maggi, C.A.; Patacchini, R.; Santicioli, P.; Lippe, I.T.; Giuliani, S.; Geppetti, P.; Bianco, E.; Selleri, S.; Meli, A. The effect of omega conotoxin GVIA, a peptide modulator of the N-type voltage sensitive calcium channels, on motor responses produced by activation of efferent and sensory nerves in mammalian smooth muscle. Naunyn Schmiedebergs Arch. Pharmacol., 1988, 338(2), 107-113.
8. Lynch, S.S.; Cheng, C.M.; Yee, J.L. Intrathecal ziconotide for refractory chronic pain. Ann. Pharmacother., 2006, 40(7-8), 1293- 1300.
9. Bowersox, S.S.; Singh, T.; Nadasdi, L.; Zukowska-Grojec, Z.; Valentino, K.; Hoffman, B.B. Cardiovascular effects of omegaconopeptides in conscious rats: mechanisms of action. J. Cardiovasc. Pharmacol., 1992, 20(5), 756-764.
10. Feng, Z.P.; Doering, C.J.; Winkfein, R.J.; Beedle, A.M.; Spafford, J.D.; Zamponi, G.W. Determinants of inhibition of transiently expressed voltage-gated calcium channels by ω-conotoxins GVIA and MVIIA. J. Biol. Chem., 2003, 278(22), 20171-20178.
11. Wermeling, D.P. Ziconotide, an intrathecally administered N-type calcium channel antagonist for the treatment of chronic pain. Pharmacotherapy, 2005, 25(8), 1084-1094.
12. McGivern, J.G. Targeting N-type and T-type calcium channels for the treatment of pain. Drug Discov. Today, 2006, 11(5-6), 245-253.
13. Wallace, M.S.; Charapata, S.G.; Fisher, R.; Byas-Smith, M.; Staats, P.S.; Mayo, M.; McGuire, D.; Ellis, D. Intrathecal ziconotide in the treatment of chronic nonmalignant pain: a randomized, doubleblind, placebo-controlled clinical trial. Neuromodulation, 2006, 9(2), 75-86.
14. Rauck, R.L.; Wallace, M.S.; Leong, M.S.; Minehart, M.; Webster, L.R.; Charapata, S.G.; Abraham, J.E.; Buffington, D.E.; Ellis, D.; Kartzinel, R. A randomized, double-blind, placebo-controlled study of intrathecal ziconotide in adults with severe chronic pain. J. Pain Symptom Manage., 2006, 31(5), 393-406.
15. Maier, C.; Gockel, H.H.; Gruhn, K.; Krumova, E.K.; Edel, M.A. Increased risk of suicide under intrathecal ziconotide treatment? - a warning. Pain, 2011, 152(1), 235-237.
16. v2.2 voltage-gated calcium channels for neuropathic pain. Biochem. Pharmacol., 2005, 70(4), 489-499.
17. Abbadie, C.; McManus, O.B.; Sun, S.Y.; Bugianesi, R.M.; Dai, G.; Haedo, R.J.; Herrington, J.B.; Kaczorowski, G.J.; Smith, M.M.; Swensen, A.M.; Warren, V.A.; Williams, B.; Arneric, S.P.; Eduljee, C.; Snutch, T.P.; Tringham, E.W.; Jochnowitz, N.; Liang, A.; Euan MacIntyre, D.; McGowan, E.; Mistry, S.; White, V.V.; Hoyt, S.B.; London, C.; Lyons, K.A.; Bunting, P.B.; Volksdorf, S.; Duffy, J.L. Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker. J. Pharmacol. Exp. Ther., 2010, 334(2), 545-555.
18. Scott, V.E.; Vortherms, T.A.; Niforatos, W.; Swensen, A.M.; Neelands, T.; Milicic, I.; Banfor, P.N.; King, A.; Zhong, C.; Simler, G.; Zhan, C.; Bratcher, N.; Boyce-Rustay, J.M.; Zhu, C.Z.; Bhatia, P.; Doherty, G.; Mack, H.; Stewart, A.O.; Jarvis, M.F. A-1048400 is a novel, orally active, state-dependent neuronal calcium channel blocker that produces dose-dependent antinociception without altering hemodynamic function in rats. Biochem. Pharmacol., 2012, 83(3), 406-418.
19. Pajouhesh, H.; Feng, Z.P.; Ding, Y.; Zhang, L.; Morrison, J.L.; Belardetti, F.; Tringham, E.; Simonson, E.; Vanderah, T.W.; Porreca, F.; Zamponi, G.W.; Mitscher, L.A.; Snutch, T.P. Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorg. Med. Chem. Lett., 2010, 20(4), 1378-1383.
20. Yamamoto, T.; Takahara, A. Recent updates of N-type calcium channel blockers with therapeutic potential for neuropathic pain and stroke. Curr. Top. Med. Chem., 2009, 9(4), 377-395.
21. Morisset, V.; Bell, D.C.; Nagy, F.; Castro, A.; Davis, J.B.; Giblin, G.M.P.; Tate, S. CNV2197944: A novel potent and selective CaV2.2 state-dependent blocker for evaluation in chronic pain. Neuroscience 2011, Washington, DC; November 12-16, 2011.
22. Ashcroft, F.M. From molecule to malady. Nature, 2006, 440(7083), 440-447.
23. Adams, P.J.; Snutch, T.P. Calcium channelopathies: voltage-gated calcium channels. Subcell. Biochem., 2007, 45, 215-251.
24. Pietrobon, D. Function and dysfunction of synaptic calcium channels: insights from mouse models. Curr. Opin. Neurobiol., 2005, 15(3), 257-265.
25. 1-42globulomer) suppress spontaneous synaptic activity by inhibition of P/Q-type calcium currents. J. Neurosci., 2008, 28(4), 788-797.
26. Mezler, M.; Barghorn, S.; Schoemaker, H.; Gross, G.; Nimmrich, V. Aβ -amyloid oligomer directly modulates P/Q-type calcium currents in Xenopus oocytes. Br. J. Pharmacol., 2012, 165(5), 1572-1583.
27. Mezler, M.; Hermann, D.; Swensen, A.M.; Draguhn, A.; Terstappen, G.C.; Gross, G.; Schoemaker, H.; Freiberg, G.; Pratt, S.; Gopalakrishnan, S.M.; Nimmrich, V. Development and validation of a fluorescence-based HTS assay for the identification of P/Q-type calcium channel blockers. Comb. Chem. High Throughput Screen., 2012, 15(5), 372-385.
28. Lam, J.K.; Jiang, X.; Hendricson, A.; Tringham, E.; Belardetti, F.; Areneric, S.P.; Snutch, T.P.; Parker, D.B. Rat Cav2.1 stable cell line expression in HEK 293 cells. SBS 13th Annual Conference 2007 (Advancing the Science of Drug Discovery: Bridging Research & Development), Montréal, Canada; April 15-19, 2007; Palais Des Congres de Montréal; Montréal, Canada; Poster number P3005.
29. Barry, P. JPCalc, a software package for calculating liquid junction potential corrections in patch-clamp, intracellular, epithelial and bilayer measurements and for correcting junction potential measurements. J. Neurosci. Methods, 1994, 51(1), 107-116.
30. Kortekaas, P.; Wadman, W.J. Development of HVA and LVA calcium currents in pyramidal CA1 neurons in the hippocampus of the rat. Brain Res. Dev. Brain Res., 1997, 101(1-2), 139-147.
31. 1A-containing high-voltageactivated calcium channels. Biophys. J., 1999, 76(3), 1384-1400.
32. 1A subunit gene generates phenotypic variants of P- and Q-type calcium channels. Nat. Neurosci., 1999, 2(5), 407-415.
33. Patil, P.G.; Brody, D.L.; Yue, D.T. Preferential closed-state inactivation of neuronal calcium channels. Neuron, 1998, 20(5), 1027-1038.
34. Gera, S.; Byerly, L. Measurement of calcium channel inactivation is dependent upon the test pulse potential. Biophys. J., 1999, 76, 3076-3088.
35. Uchitel, O.D.; Di Guilmi, M.N.; Urbano, F.J.; Gonzalez-Inchauspe, C. Acute modulation of calcium currents and synaptic transmission by gabapentinoids. Channels (Austin), 2010, 4(6), 490-496.
36. Nordin, M.; Nystrom, B.; Wallin, U.; Hagbarth, K.E. Ectopic sensory discharges and paresthesiae in patients with disorders of peripheral nerves, dorsal roots and dorsal columns. Pain, 1984, 20(3), 231-245.
37. Tottene, A.; Conti, R.; Fabbro, A.; Vecchia, D.; Shapovalova, M.; Santello, M.; van den Maagdenberg, A.M.; Ferrari, M.D.; Pietrobon, D. Enhanced excitatory transmission at cortical synapses as the basis for facilitated spreading depression in Ca(v)2.1 knockin migraine mice. Neuron, 2009, 61(5), 762-773.
38. Dai, G.; Haedo, R.J.; Warren, V.A.; Ratliff, K.S.; Bugianesi, R.M.; Rush, A.; Williams, M.E.; Herrington, J.; Smith, M.M.; McManus, O.B.; Swensen, A.M. 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.
39. Bezprozvanny, I.; Scheller, R.H.; Tsien, R.W. Functional impact of syntaxin on gating of N-type and Q-type calcium channels. Nature, 1995, 378(6557), 623-626.
40. Degtiar, V.E.; Scheller, R.H.; Tsien, R.W. Syntaxin modulation of slow inactivation of N-type calcium channels. J. Neurosci., 2000, 20(12), 4355-4367.
41. Mintz, I.M.; Adams, M.E.; Bean, B.P. P-type calcium channels in rat central and peripheral neurons. Neuron, 1992, 9(1), 85-95.
42. Yan, Z.; Chi, P.; Bibb, J.A.; Ryan, T.A.; Greengard, P. Roscovitine: a novel regulator of P/Q-type calcium channels and transmitter release in central neurons. J. Physiol., 2002, 540(3), 761-770.
43. Finley, M.F.; Lubin, M.L.; Neeper, M.P.; Beck, E.; Liu, Y.; Flores, C.M.; Qin, N. An integrated multiassay approach to the discovery of small-molecule N-type voltage-gated calcium channel antagonists. Assay Drug Dev. Technol., 2010, 8, 685-694.
44. Swensen, A.M.; Niforatos, W.; Vortherms, T.A.; Perner, R.J.; Li, T.; Schrimpf, M.R.; Scott, V.E.; Lee, L.; Jarvis, M.F.; McGaraughty, S. An automated electrophysiological assay for differentiating ca(v)2.2 inhibitors based on state dependence and kinetics. Assay Drug Dev. Technol., 2012, 10, 542-550.