High-throughput screen for small molecule inhibitors of Mint1-PDZ domains

Assay and Drug Development Technologies

Volumn 5, Issue 6, 2007, Pages 769-783

  Chen, Xuesong ^a   Longgood, Jamie C ^a   Michnoff, Carolyn ^a   Wei, Shuguang ^a   Frantz, Doug E ^a   Bezprozvanny, Llya ^a  

^a UNIVERSITY OF TEXAS SOUTHWESTERN MEDICAL CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CALCIUM CHANNEL N TYPE; GLUTATHIONE TRANSFERASE; PDZ PROTEIN; PROTEIN INHIBITOR;

AMPLIFIED LUMINESCENT PROXIMITY HOMOGENEOUS ASSAY; ARTICLE; DRUG DETERMINATION; FLUORESCENCE RESONANCE ENERGY TRANSFER; HIGH THROUGHPUT SCREENING; LUMINESCENCE;

ADAPTOR PROTEINS, SIGNAL TRANSDUCING; AMINO ACID SEQUENCE; ANIMALS; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; ESCHERICHIA COLI; FLUORESCENCE RESONANCE ENERGY TRANSFER; GLUTATHIONE TRANSFERASE; INDICATORS AND REAGENTS; LIGHT; LUMINESCENCE; MEMBRANE PROTEINS; OXYGEN; PDZ DOMAINS; RATS; REACTIVE OXYGEN SPECIES; RECOMBINANT PROTEINS; STREPTAVIDIN; SUBSTRATE SPECIFICITY;

EID: 38049083087     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2007.092     Document Type: Article

References (42)

1. Kornau HC, Seeburg PH, Kennedy MB: Interaction of ion channels and receptors with PDZ domain proteins. Curr Opin Neurobiol 1997;7:368-373.
2. Ponting CP, Phillips C, Davies KE, Blake DJ: PDZ domains: targeting signalling molecules to sub-membranous sites. Bioessays 1997;19:469-479.
3. Fanning AS, Anderson JM: Protein-protein interactions: PDZ domain networks. Curr Biol 1996;6:1385-1388.
4. Sheng M, Wyszynski M: Ion channel targeting in neurons. Bioessays 1997;19:847-853.
5. Doyle DA, Lee A, Lewis J, Kim E, Sheng M, MacKinnon R: Crystal structures of a complexed and peptide-free membrane protein-binding domain: molecular basis of peptide recognition by PDZ. Cell 1996;85:1067-1076.
6. Daniels DL, Cohen AR, Anderson JM, Brunger AT: Crystal structure of the hCASK PDZ domain reveals the structural basis of class II PDZ domain target recognition. Nat Struct Biol 1998;5:317-325.
7. Morais Cabral JH, Petosa C, Sutcliffe MJ, Raza S, Byron O, Poy F, et al.: Crystal structure of a PDZ domain. Nature 1996;382:649-652.
8. Bezprozvanny I, Maximov A: Classification of PDZ domains. FEBS Lett 2001;509:457-462.
9. Cui H, Hayashi A, Sun HS, Belmares MP, Cobey C, Phan T, et al.: PDZ protein interactions underlying NMDA receptor-mediated excitotoxicity and neuroprotection by PSD-95 inhibitors. J Neurosci 2007;27:9901-9915.
10. Yaksh TL: Spinal systems and pain processing: development of novel analgesic drugs with mechanistically defined models. Trends Pharmacol Sci 1999;20:329-337.
11. McCleskey EW, Gold MS: Ion channels of nociception. Annu Rev Physiol 1999;61:835-856.
12. 125I]omega-conotoxin in rat brain. Eur J Pharmacol 1988;146:181-183.
13. Gohil K, Bell JR, Ramachandran J, Miljanich GP: Neuroanatomical distribution of receptors for a novel voltage-sensitive calcium-channel antagonist, SNX-230 (omega-conopeptide MVIIC). Brain Res 1994;653:258-266.
14. 2+ channel subtypes on rat spinal motor neurons, interneurons, and nerve terminals. J Neurosci 1998;18:6319-6330.
15. Malmberg AB, Yaksh TL: Effect of continuous intrathecal infusion of omega-conopeptides, N-type calcium-channel blockers, on behavior and antinociception in the formalin and hot-plate tests in rats. Pain 1995;60:83-90.
16. Malmberg AB, Yaksh TL: Voltage-sensitive calcium channels in spinal nociceptive processing: blockade of N- and P-type channels inhibits formalin-induced nociception. J Neurosci 1994;14:4882-4890.
17. 1B subunit of the voltage-dependent calcium channel. Mol Cell Neurosci 2001;18:235-245.
18. 2+ channel. EMBO J 2001;20:2349-2356.
19. 2+ channels. Neuroreport 2001;12:2423-2427.
20. Altier C, Dale CS, Kisilevsky AE, Chapman K, Castiglioni AJ, Matthews EA, et al.: Differential role of N-type calcium channel splice isoforms in pain. J Neurosci 2007;27:6363-6373.
21. Penn RD, Paice JA: Adverse effects associated with the intrathecal administration of ziconotide. Pain 2000;85:291-296.
22. Brose WG, Gutlove DP, Luther RR, Bowersox SS, McGuire D: Use of intrathecal SNX-111, a novel, N-type, voltage-sensitive, calcium channel blocker, in the management of intractable brachial plexus avulsion pain. Clin J Pain 1997;13:256-259.
23. McGivern JG: Targeting N-type and T-type calcium channels for the treatment of pain. Drug Discov Today 2006;11:245-253.
24. 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.
25. Maximov A, Sudhof TC, Bezprozvanny I: Association of neuronal calcium channels with modular adaptor proteins. J Biol Chem 1999;274:24453-24456.
26. Long JF, Feng W, Wang R, Chan LN, Ip FC, Xia J, et al.: Autoinhibition of X11/Mint scaffold proteins revealed by the closed conformation of the PDZ tandem. Nat Struct Mol Biol 2005;12:722-728.
27. Maximov A, Bezprozvanny I: Synaptic targeting of N-type calcium channels in hippocampal neurons. J Neurosci 2002;22:6939-6952.
28. Wu X, Glickman JF, Bowen BR, Sills MA: Comparison of assay technologies for a nuclear receptor assay screen reveals differences in the sets of identified functional antagonists. J Biomol Screen 2003;8:381-392.
29. Glickman JF, Wu X, Mercuri R, Illy C, Bowen BR, He Y, et al.: A comparison of ALPHAScreen, TR-FRET, and TRF as assay methods for FXR nuclear receptors. J Biomol Screen 2002;7:3-10.
30. Wu X, Sills MA, Zhang JH: Further comparison of primary hit identification by different assay technologies and effects of assay measurement variability. J Biomol Screen 2005;10:581-589.
31. Morrison LE: Time-resolved detection of energy transfer: theory and application to immunoassays. Anal Biochem 1988;174:101-120.
32. Imbert PE, Unterreiner V, Siebert D, Gubler H, Parker C, Gabriel D: Recommendations for the reduction of compound artifacts in time-resolved fluorescence resonance energy transfer assays. Assay Drug Dev Technol 2007;5:363-372.
33. Ullman EF, Kirakossian H, Singh S, Wu ZP, Irvin BR, Pease JS, et al.: Luminescent oxygen channeling immunoassay: measurement of particle binding kinetics by chemiluminescence. Proc Natl Acad Sci USA 1994;91:5426-5430.
34. 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.
35. Cooper MA: Label-free screening of bio-molecular interactions. Anal Bioanal Chem 2003;377:834-842.
36. Feng BY, Shoichet BK: A detergent-based assay for the detection of promiscuous inhibitors. Nat Protoc 2006;1:550-553.
37. Tsunoda S, Sierralta J, Sun Y, Bodner R, Suzuki E, Becker A, et al.: A multivalent PDZ-domain protein assembles signalling complexes in a G-protein-coupled cascade. Nature 1997;388:243-249.
38. Fanning AS, Anderson JM: PDZ domains: fundamental building blocks in the organization of protein complexes at the plasma membrane. J Clin Invest 1999;103:767-772.
39. Dev KK: Making protein interactions druggable: targeting PDZ domains. Nat Rev Drug Discov 2004;3:1047-1056.
40. Joshi M, Vargas C, Boisguerin P, Diehl A, Krause G, Schmieder P, et al.: Discovery of low-molecular-weight ligands for the AF6 PDZ domain. Angew Chem Int Ed Engl 2006;45:3790-3795.
41. Wen W, Wang W, Zhang M: Targeting PDZ domain proteins for treating NMDA receptor-mediated excitotoxicity. Curr Top Med Chem 2006;6:711-721.
42. Shan J, Shi DL, Wang J, Zheng J: Identification of a specific inhibitor of the dishevelled PDZ domain. Biochemistry 2005;44:15495-15503.