Development and validation of a cell-based high-throughput screening assay for TRPM2 channel modulators

Journal of Biomolecular Screening

Volumn 13, Issue 1, 2008, Pages 54-61

  Song, Yumei ^a   Buelow, Ben ^a   Perraud, Anne Laure ^b   Scharenberg, Andrew M ^a  

^a UNIVERSITY OF WASHINGTON   (United States)

^b UNIVERSITY OF COLORADO   (United States)

Author keywords

Cell based assay; DT40 control cell line; DT40 TRPM2 cell line; Fluorescence Ca2+ probe; High throughput screening; TRPM2 ion channels

Indexed keywords

2 (4 METHYLPIPERAZIN 1 YL) 5H BENZO(1,5)NAPHTHYRIDIN 6 ONE; CALCIUM ION; FLUORESCENT DYE; GPI 16539; HYDROGEN PEROXIDE; N (4 AMYLCINNAMOUS)ANTHRANILIC ACID; NITROSOGUANIDINE; PROTEIN INHIBITOR; TRANSIENT RECEPTOR POTENTIAL CHANNEL M; TRANSIENT RECEPTOR POTENTIAL CHANNEL M2; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; B LYMPHOCYTE; CELL ASSAY; CELL LINE; CELL SUSPENSION; CHANNEL GATING; CONTROLLED STUDY; EMBRYO; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; STATISTICAL ANALYSIS; VALIDATION STUDY;

ANILINE COMPOUNDS; ANIMALS; CELL LINE; CHICKENS; DRUG EVALUATION, PRECLINICAL; FLUORESCENT DYES; HUMANS; KINETICS; RECOMBINANT PROTEINS; TRANSFECTION; TRPM CATION CHANNELS; XANTHENES;

ANIMALIA;

EID: 37749036756     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057107310986     Document Type: Article

References (23)

1. Montell C.: The TRP superfamily of cation channels. Sci STKE 2005 ; 2005: re3.
2. Perraud AL, Fleig A., Dunn CA, Bagley LA, Launay P., Schmitz C.,, et al. ADP-ribose gating of the calcium-permeable LTRPC2 channel revealed by Nudix motif homology. Nature 2001 ; 411: 595-599.
3. Sano Y., Inamura K., Miyake A., Mochizuki S., Yokoi H., Matsushime H.,, et al. Immunocyte Ca2+ influx system mediated by LTRPC2. Science 2001 ; 293: 1327-1330.
4. Perraud AL, Takanishi CL, Shen B., Kang S., Smith MK, Schmitz C.,, et al. Accumulation of free ADP-ribose from mitochondria mediates oxidative stress-induced gating of TRPM2 cation channels. J Biol Chem 2005 ; 280: 6138-6148.
5. Perraud AL, Schmitz C., Scharenberg AM: TRPM2 Ca2+ permeable cation channels: from gene to biological function. Cell Calcium 2003 ; 33: 519-531.
6. Hara Y., Wakamori M., Ishii M., Maeno E., Nishida M., Yoshida T.,, et al. LTRPC2 Ca2+-permeable channel activated by changes in redox status confers susceptibility to cell death. Mol Cell 2002 ; 9: 163-173.
7. Wehage E., Eisfeld J., Heiner I., Jungling E., Zitt C., Luckhoff A.: Activation of the cation channel long transient receptor potential channel 2 (LTRPC2) by hydrogen peroxide: a splice variant reveals a mode of activation independent of ADP-ribose. J Biol Chem 2002 ; 277: 23150-23156.
8. Perraud AL, Shen B., Dunn CA, Rippe K., Smith MK, Bessman MJ,, et al. NUDT9, a member of the Nudix hydrolase family, is an evolutionarily conserved mitochondrial ADP-ribose pyrophosphatase. J Biol Chem 2003 ; 278: 1794-1801.
9. Shen BW, Perraud AL, Scharenberg A., Stoddard BL: The crystal structure and mutational analysis of human NUDT9. J Mol Biol 2003 ; 332: 385-398.
10. Kraft R., Grimm C., Grosse K., Hoffmann A., Sauerbruch S., Kettenmann H.,, et al. Hydrogen peroxide and ADP-ribose induce TRPM2-mediated calcium influx and cation currents in microglia. Am J Physiol Cell Physiol 2004 ; 286: C129 - C137.
11. Perraud AL, Knowles HM, Schmitz C.: Novel aspects of signaling and ion-homeostasis regulation in immunocytes: the TRPM ion channels and their potential role in modulating the immune response. Mol Immunol 2004 ; 41: 657-673.
12. Inamura K., Sano Y., Mochizuki S., Yokoi H., Miyake A., Nozawa K.,, et al. Response to ADP-ribose by activation of TRPM2 in the CRI-G1 insulinoma cell line. J Membr Biol 2003 ; 191: 201-207.
13. Fonfria E., Marshall IC, Benham CD, Boyfield I., Brown JD, Hill K.,, et al. TRPM2 channel opening in response to oxidative stress is dependent on activation of poly(ADP-ribose) polymerase. Br J Pharmacol 2004 ; 143: 186-192.
14. Zhang JH, Chung TD, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high-throughput screening assays. J Biomol Screen 1999 ; 4: 67-73.
15. Ferraris D., Ko YS, Pahutski T., Ficco RP, Serdyuk L., Alemu C.,, et al. Design and synthesis of poly ADP-ribose polymerase-1 inhibitors: 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries. J Med Chem 2003 ; 46: 3138-3151.
16. Iversen PW, Eastwood BJ, Sittampalam GS, Cox KL: A comparison of assay performance measures in screening assays: signal window, Z′ factor, and assay variability ratio. J Biomol Screen 2006 ; 11: 247-252.
17. Togashi K., Hara Y., Tominaga T., Higashi T., Konishi Y., Mori Y.,, et al. TRPM2 activation by cyclic ADP-ribose at body temperature is involved in insulin secretion. Embo J 2006 ; 25: 1804-1815.
18. Kraft R., Grimm C., Frenzel H., Harteneck C.: Inhibition of TRPM2 cation channels by N-(p-amylcinnamoyl)anthranilic acid. Br J Pharmacol 2006 ; 148: 264-273.
19. Veal EA, Day AM, Morgan BA: Hydrogen peroxide sensing and signaling. Mol Cell 2007 ; 26: 1-14.
20. Ding J., Takano T., Gao S., Han W., Noda C., Yanagi S.,, et al. Syk is required for the activation of Akt survival pathway in B cells exposed to oxidative stress. J Biol Chem 2000 ; 275: 30873-30877.
21. Immenschuh S., Baumgart-Vogt E.: Peroxiredoxins, oxidative stress, and cell proliferation. Antioxid Redox Signal 2005 ; 7: 768-777.
22. Hidalgo C., Donoso P., Carrasco MA: The ryanodine receptors Ca2+ release channels: cellular redox sensors? IUBMB Life 2005 ; 57: 315-322.
23. Tohyama Y., Takano T., Yamamura H.: B cell responses to oxidative stress. Curr Pharm Des 2004 ; 10: 835-839.