Time-resolved fluorescence resonance energy transfer assay for discovery of small-molecule inhibitors of methyl-CpG binding domain protein 2

Journal of Biomolecular Screening

Volumn 19, Issue 7, 2014, Pages 1060-1069

  Wyhs, Nicolas ^a   Walker, David ^a   Giovinazzo, Hugh ^a   Yegnasubramanian, Srinivasan ^b   Nelson, William G ^a,b  

^a JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b JOHNS HOPKINS UNIVERSITY   (United States)

Author keywords

DNA protein interaction inhibitor; fluorescence polarization; high throughput screening assay; MBD2; MBD2 small molecule inhibitor; methylated CpG binding domain protein 2; time resolved fluorescence resonance energy transfer; TR FRET

Indexed keywords

AURINTRICARBOXYLIC ACID; DOUBLE STRANDED DNA; IDARUBICIN; METHYL CPG BINDING PROTEIN 2; MITOXANTRONE; PENTOXYVERINE; PURINERGIC P2X1 RECEPTOR; SURAMIN; 4,4,',4'',4'''-(CARBONYLBIS(IMINO-5,1,3-BENZENETRIYLBIS(CARBONYLIMINO)))TETRAKIS(BENZENE-1,3-DISULFONATE); BENZENESULFONIC ACID DERIVATIVE; DNA; DNA BINDING PROTEIN; FLUORESCENT DYE; MBD2 PROTEIN, HUMAN; OLIGONUCLEOTIDE; PROTEIN BINDING; SP1 PROTEIN, HUMAN; TRANSCRIPTION FACTOR SP1;

ARTICLE; CONTROLLED STUDY; DNA METHYLATION; DNA TRANSCRIPTION; DOSE RESPONSE; FLUORESCENCE POLARIZATION; FLUORESCENCE RESONANCE ENERGY TRANSFER; HIGH THROUGHPUT SCREENING; HUMAN; IC 50; PRIORITY JOURNAL; PROTEIN DNA INTERACTION; PROTEIN DOMAIN; PROTEIN NUCLEIC ACID INTERACTION; SIGNAL NOISE RATIO; TIME RESOLVED FLUORESCENCE RESONANCE ENERGY TRANSFER ASSAY; TUMOR SUPPRESSOR GENE; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG DEVELOPMENT; PRECLINICAL STUDY; PROCEDURES;

AURINTRICARBOXYLIC ACID; BENZENESULFONATES; DNA; DNA METHYLATION; DNA-BINDING PROTEINS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; FLUORESCENCE RESONANCE ENERGY TRANSFER; FLUORESCENT DYES; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; IDARUBICIN; MITOXANTRONE; OLIGONUCLEOTIDES; PROTEIN BINDING; SP1 TRANSCRIPTION FACTOR;

EID: 84904599346     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057114526433     Document Type: Article

References (31)

1. Baylin S. B., Jones P. A.. A Decade of Exploring the Cancer Epigenome: Biological and Translational Implications. Nat. Rev. 2011 ; 11: 726-734
2. Lai A. Y., Wade P. A.. Cancer Biology and NuRD: A Multifaceted Chromatin Remodelling Complex. Nat. Rev. 2011 ; 11: 588-596
3. Cameron E. E., Bachman K. E., Myohanen S., et al. Synergy of Demethylation and Histone Deacetylase Inhibition in the Re-expression of Genes Silenced in Cancer. Nat. Genet. 1999 ; 21: 103-107
4. Foulks J. M., Parnell K. M., Nix R. N., et al. Epigenetic Drug Discovery: Targeting DNA Methyltransferases. J. Biomol. Screen. 2012 ; 17: 2-17
5. Mahindra A., Laubach J., Raje N., et al. Latest Advances and Current Challenges in the Treatment of Multiple Myeloma. Nat. Rev. 2012 ; 9: 135-143
6. Rius M., Lyko F.. Epigenetic Cancer Therapy: Rationales, Targets and Drugs. Oncogene. 2012 ; 31: 4257-4265
7. Lin X., Nelson W. G.. Methyl-CpG-Binding Domain Protein-2 Mediates Transcriptional Repression Associated with Hypermethylated GSTP1 CpG Islands in MCF-7 Breast Cancer Cells. Cancer Res. 2003 ; 63: 498-504
8. Su L. K., Kinzler K. W., Vogelstein B., et al. Multiple Intestinal Neoplasia Caused by a Mutation in the Murine Homolog of the APC Gene. Science. 1992 ; 256: 668-670
9. Sansom O. J., Berger J., Bishop S. M., et al. Deficiency of Mbd2 Suppresses Intestinal Tumorigenesis. Nat. Genet. 2003 ; 34: 145-147
10. Fernandes P. B.. Technological Advances in High-Throughput Screening. Curr. Opin. Chem. Biol. 1998 ; 2: 597-603
11. Liu B., Li S., Hu J.. Technological Advances in High-Throughput Screening. Am. J. Pharmacogenomics. 2004 ; 4: 263-276
12. Gribbon P., Sewing A.. Fluorescence Readouts in HTS: No Gain without Pain?. Drug Discov. Today. 2003 ; 8: 1035-1043
13. Bazin H., Trinquet E., Mathis G.. Time Resolved Amplification of Cryptate Emission: A Versatile Technology to Trace Biomolecular Interactions. J. Biotechnol. 2002 ; 82: 233-250
14. Owicki J. C.. Fluorescence Polarization and Anisotropy in High Throughput Screening: Perspectives and Primer. J. Biomol. Screen. 2000 ; 5: 297-306
15. Yegnasubramanian S., Lin X., Haffner M. C., et al. Combination of Methylated-DNA Precipitation and Methylation-Sensitive Restriction Enzymes (COMPARE-MS) for the Rapid, Sensitive and Quantitative Detection of DNA Methylation. Nucleic Acids Res. 2006 ; 34: e19
16. R: A Language and Environment for Statistical Computing. Vienna, Austria: R Foundation for Statistical Computing ; 2011 :
17. Zhang J. H., Chung T. D., Oldenburg K. R.. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. J. Biomol. Screen. 1999 ; 4: 67-73
18. Chan L. L., Pineda M., Heeres J. T., et al. A General Method for Discovering Inhibitors of Protein-DNA Interactions Using Photonic Crystal Biosensors. ACS Chem. Biol. 2008 ; 3: 437-448
19. Dawson K. M.. Activity of SC33428, a Novel Bishydrazone-Bridged Derivative of 4-Demethoxydaunorubicin, against Experimental Tumors in Mice. Cancer Res. 1983 ; 43: 2880-2883
20. Shenkenberg T. D., Von Hoff D. D.. Mitoxantrone: A New Anticancer Drug with Significant Clinical Activity. Ann. Intern. Med. 1986 ; 105: 67-81
21. Blumenthal T., Landers T. A.. The Inhibition of Nucleic Acid-Binding Proteins by Aurintricarboxylic Acid. Biochem. Biophys. Res. Commun. 1973 ; 55: 680-688
22. Hausmann R., Schmalzing G.. P2X1 and P2X2 Receptors in the Central Nervous System as Possible Drug Targets. CNS Neurol. Disord. Drug Targets. 2012 ; 11: 675-686
23. Hulsmann M., Nickel P., Kassack M., et al. NF449, a Novel Picomolar Potency Antagonist at Human P2X1 Receptors. Eur. J. Pharmacol. 2003 ; 470: 1-7
24. Oka S., Shiraishi Y., Yoshida T., et al. NMR Structure of Transcription Factor Sp1 DNA Binding Domain. Biochemistry. 2004 ; 43: 16027-16035
25. Ho K. L., McNae I. W., Schmiedeberg L., et al. MeCP2 Binding to DNA Depends upon Hydration at Methyl-CpG. Mol. Cell. 2008 ; 29: 525-531
26. El-Ajouz S., Ray D., Allsopp R. C., et al. Molecular Basis of Selective Antagonism of the P2X1 Receptor for ATP by NF449 and Suramin: Contribution of Basic Amino Acids in the Cysteine-Rich Loop. Br. J. Pharmacol. 2012 ; 165: 390-400
27. North R. A.. Molecular Physiology of P2X Receptors. Physiol. Rev. 2002 ; 82: 1013-1067
28. Burnstock G.. Pathophysiology and Therapeutic Potential of Purinergic Signaling. Pharmacol. Rev. 2006 ; 58: 58-86
29. Hohenegger M., Waldhoer M., Beindl W., et al. Gsalpha-Selective G Protein Antagonists. Proc. Natl. Acad. Sci. U.S.A. 1998 ; 95: 346-351
30. Krejci P., Murakami S., Prochazkova J., et al. NF449 Is a Novel Inhibitor of Fibroblast Growth Factor Receptor 3 (FGFR3) Signaling Active in Chondrocytes and Multiple Myeloma Cells. J. Biol. Chem. 2010 ; 285: 20644-20653
31. Scarsdale J. N., Webb H. D., Ginder G. D., et al. Solution Structure and Dynamic Analysis of Chicken MBD2 Methyl Binding Domain Bound to a Target-Methylated DNA Sequence. Nucleic Acids Res. 2011 ; 39: 6741-6752