Novel Neuroprotective K+ Channel Inhibitor Identified by High-Throughput Screening in Yeast

Molecular Pharmacology

Volumn 65, Issue 1, 2004, Pages 214-219

  Zaks Makhina, Elena ^a   Kim, Yonjung ^a   Aizenman, Elias ^a   Levitan, Edwin S ^a  

^a UNIVERSITY OF PITTSBURGH SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 BICYCLO[2.2.1]HEPT 2 YL BENZENE 1,2 DIOL; BENZENE DERIVATIVE; COMPOUND 48F10; NEUROPROTECTIVE AGENT; NORBORNANE DERIVATIVE; POTASSIUM CHANNEL; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL KIR2.1 BLOCKING AGENT; TETRYLAMMONIUM; UNCLASSIFIED DRUG;

ANIMAL CELL; APOPTOSIS; ARTICLE; BIOASSAY; BRAIN PROTECTION; CELL STRAIN; COMBINATORIAL CHEMISTRY; CONTROLLED STUDY; DRUG DETERMINATION; DRUG IDENTIFICATION; DRUG MECHANISM; ELECTROPHYSIOLOGY; FUNGUS GROWTH; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; MAMMAL CELL; NERVE CELL NECROSIS; NONHUMAN; PATCH CLAMP; POTASSIUM CHANNEL KIR2.1; POTASSIUM CHANNEL KV2.1; PRIORITY JOURNAL; RAT; SACCHAROMYCES CEREVISIAE; YEAST;

ANIMALS; BICYCLO COMPOUNDS; CELLS, CULTURED; DELAYED RECTIFIER POTASSIUM CHANNELS; DRUG EVALUATION, PRECLINICAL; HUMANS; NEUROPROTECTIVE AGENTS; POTASSIUM CHANNEL BLOCKERS; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; RATS; RATS, SPRAGUE-DAWLEY; SACCHAROMYCES CEREVISIAE; SHAB POTASSIUM CHANNELS; TETRAETHYLAMMONIUM;

EID: 1642576972     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.65.1.214     Document Type: Article

References (28)

1. Aizenman E, Stout AK, Hartnett KA, Dineley KE, McLaughlin B, and Reynolds IJ (2000) Induction of neuronal apoptosis by thiol oxidation: putative role of intracellular zinc release. J Neurochem 75:1878-1888.
2. Bretschneider F, Wrisch A, Lehmann-Horn F, and Grissmer S (1999) External tetraethylammonium as a molecular caliper for sensing the shape of the outer vestibule of potassium channels. Biophys J 76:2351-2360.
3. Erdelyi L and Such G (1988) The A-type potassium current: catechol-induced blockage in snail neurons. Neurosci Lett 92:46-51.
4. Fedida D, Maruoka ND, and Lin S (1999) Modulation of slow inactivation in human cardiac Kv1.5 channels by extra- and intracellular permeant cations. J Physiol (Lond) 515:315-329.
5. Gaber RF, Styles CA, and Fink GR (1988) TRK1 encodes a plasma membrane protein required for high-affinity potassium transport in Saccharomyces cerevisiae. Mol Cell Biol 8:2848-2859.
6. Hahnenberger KM, Krystal M, Esposito K, Tang W, and Kurtz S (1996) Use of microphysiometry for analysis of heterologous ion channels expressed in yeast. Nat Biotechnol 14:880-883.
7. Hahnenberger KM and Kurtz SE (1997) A drug screening program for ion channels expressed in yeast. Trends Biotechnol 15:1-4.
8. +-free solutions in rat cortical neurons in vitro. J Neurochem 68:1836-1845.
9. Hess D and El Manira A (2001) Characterization of a high-voltage-activated IA current with a role in spike timing and locomotor pattern generation. Proc Natl Acad Sci USA 98:5276-5281.
10. Ito I and Maeno T (1986) Catechol: a potent and specific inhibitor of the fast potassium channel in frog primary afferent neurones. J Physiol (Lond) 373:115-127.
11. + transport in Saccharomyces cerevisiae. Genetics 125:305-312.
12. + channels in motor pattern generation in the Xenopus embryo. J Neurosci 18:1602-1612.
13. Lopatin AN, Makhina EN, and Nichols CG (1995) The mechanism of inward rectification of potassium channels: "long-pore plugging" by cytoplasmic polyamines. J Gen Physiol 106:923-955.
14. Ma T, Vetrivel L, Yang H, Pedemonte N, Zegarra-Moran O, Galietta LJ, and Verkman AS (2002) High-affinity activators of cystic fibrosis transmembrane conductance regulator (CFTR) chloride conductance identified by high-throughput screening. J Biol Chem 277:37235-37241.
15. McLaughlin B, Pal S, Tran MP, Parsons AA, Barone FC, Erhardt JA, and Aizenman E (2001) p38 activation is required upstream of potassium current enhancement and caspase cleavage in thiol oxidant-induced neuronal apoptosis. J Neurosci 21:3303-3311.
16. Minor DL Jr, Masseling SJ, Jan YN, and Jan LY (1999) Transmembrane structure of an inwardly rectifying potassium channel. Cell 96:879-891.
17. Pal S, Hartnett KA, Nerbonne JM, Levitan ES, and Aizenman E (2003) Mediation of neuronal apoptosis by Kv2.1-encoded potassium channels. J Neurosci 23:4798-4802.
18. Sentenac H, Bonneaud N, Minet M, Lacroute F, Salmon JM, Gaymard F, and Grignon C (1992) Cloning and expression in yeast of a plant potassium ion transport system. Science (Wash DC) 256:663-665.
19. Tang W, Ruknudin A, Yang WP, Shaw SY, Knickerbocker A, and Kurtz S (1995) Functional expression of a vertebrate inwardly rectifying K+ channel in yeast. Mol Biol Cell 6:1231-1240.
20. Wang X, Xiao AY, Ichinose T, and Yu SP (2000) Effects of tetraethylammonium analogs on apoptosis and membrane currents in cultured cortical neurons. J Pharmacol Exp Ther 295:524-530.
21. + channels as therapeutic drug targets. Pharmacol Ther 94:157-182.
22. Willumsen NJ, Bech M, Olesen SP, Jensen BS, Korsgaard MP, and Christophersen P (2003) High throughput electrophysiology: new perspectives for ion channel drug discovery. Receptors Channels 9:3-12.
23. Worley JF 3rd and Main MJ (2002) An industrial perspective on utilizing functional ion channel assays for high throughput screening. Recept Channels 8:269-282.
24. Xie LH, John SA, and Weiss JN (2003) Inward rectification by polyamines in mouse Kir2.1 channels: synergy between blocking components. J Physiol (Lond) 550:67-82.
25. + channel. Neuron 14:1047-1054.
26. Yi BA, Lin YF, Jan YN, and Jan LY (2001) Yeast screen for constitutively active mutant G protein-activated potassium channels. Neuron 29:657-667.
27. Yu SP, Canzoniero LM, and Choi DW (2001) Ion homeostasis and apoptosis. Curr Opin Cell Biol 13:405-411.
28. Yu SP, Yeh CH, Sensi SL, Gwag BJ, Canzoniero LM, Farhangrazi ZS, Ying HS, Tian M, Dugan LL, and Choi DW (1997) Mediation of neuronal apoptosis by enhancement of outward potassium current. Science (Wash DC) 278:114-117.