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Volumn 20, Issue 6, 2015, Pages 810-820

A high-throughput mass spectrometry assay coupled with redox activity testing reduces artifacts and false positives in lysine demethylase screening

Author keywords

epigenetics; KDM1A or LSD1 or AOF2; KDM4C or JMJD2C or GASC1; lysine demethylase (KDM); redox; self assembled monolayer desorption ionization mass spectrometry (SAMDI)

Indexed keywords

2 OXOGLUTARIC ACID; 4 CARBOXY 2,2' DIPYRIDINE; ENZYME INHIBITOR; EPZ 020809; HISTONE DEMETHYLASE; LYSINE DEMETHYLASE; LYSINE DEMETHYLASE INHIBITOR; LYSINE SPECIFIC DEMETHYLASE 1; LYSINE SPECIFIC DEMETHYLASE 4C; N OXAYLGLYCINE; PROTEIN AOF2; PROTEIN GASC1; PROTEIN JMJD2C; PROTEIN LSD1; PYRIDINE DERIVATIVE; TRANYLCYPROMINE; UNCLASSIFIED DRUG; HISTONE; KDM1A PROTEIN, HUMAN; KDM4C PROTEIN, HUMAN; MOLECULAR LIBRARY;

EID: 84931426731     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057115575689     Document Type: Article
Times cited : (34)

References (35)
  • 1
    • 79960367903 scopus 로고    scopus 로고
    • Chemogenetic Analysis of Human Protein Methyltransferases
    • Richon V. M., Johnston D., Sneeringer C. J., et al. Chemogenetic Analysis of Human Protein Methyltransferases. Chem. Biol. Drug. Des. 2011 ; 78: 199-210
    • (2011) Chem. Biol. Drug. des , vol.78 , pp. 199-210
    • Richon, V.M.1    Johnston, D.2    Sneeringer, C.J.3
  • 2
    • 84860371953 scopus 로고    scopus 로고
    • Epigenetic Protein Families: A New Frontier for Drug Discovery
    • Arrowsmith C. H., Bountra C., Fish P. V., et al. Epigenetic Protein Families: A New Frontier for Drug Discovery. Nat. Rev. Drug Discov. 2012 ; 11: 384-400
    • (2012) Nat. Rev. Drug Discov , vol.11 , pp. 384-400
    • Arrowsmith, C.H.1    Bountra, C.2    Fish, P.V.3
  • 3
    • 84878872227 scopus 로고    scopus 로고
    • Drugging the Human Methylome: An Emerging Modality for Reversible Control of Aberrant Gene Transcription
    • Wigle T. J., Copeland R. A.. Drugging the Human Methylome: An Emerging Modality for Reversible Control of Aberrant Gene Transcription. Curr. Opin. Chem. Biol. 2013 ; 17: 369-378
    • (2013) Curr. Opin. Chem. Biol , vol.17 , pp. 369-378
    • Wigle, T.J.1    Copeland, R.A.2
  • 4
    • 84890284556 scopus 로고    scopus 로고
    • Molecular Pathways: Protein Methyl-transferases in Cancer
    • Copeland R. A.. Molecular Pathways: Protein Methyl-transferases in Cancer. Clin. Cancer Res. 2013 ; 19: 6344-6350
    • (2013) Clin. Cancer Res , vol.19 , pp. 6344-6350
    • Copeland, R.A.1
  • 5
    • 16344368814 scopus 로고    scopus 로고
    • Histone Demethylation Catalysed by LSD1 is a Flavin-Dependent Oxidative Process
    • Forneris F., Binda C., Vanoni M. A., et al. Histone Demethylation Catalysed by LSD1 Is a Flavin-Dependent Oxidative Process. FEBS Lett. 2005 ; 579: 2203-2207
    • (2005) FEBS Lett , vol.579 , pp. 2203-2207
    • Forneris, F.1    Binda, C.2    Vanoni, M.A.3
  • 7
    • 32844454603 scopus 로고    scopus 로고
    • Histone Demethylation by a Family of JmjC Domain-Containing Proteins
    • Tsukada Y., Fang J., Erdjument-Bromage H., et al. Histone Demethylation by a Family of JmjC Domain-Containing Proteins. Nature. 2006 ; 439: 811-816
    • (2006) Nature , vol.439 , pp. 811-816
    • Tsukada, Y.1    Fang, J.2    Erdjument-Bromage, H.3
  • 8
    • 0034282790 scopus 로고    scopus 로고
    • Identification of a Novel Gene, GASC1, within an Amplicon at 9p23-24 Frequently Detected in Esophageal Cancer Cell Lines
    • Yang Z. Q., Imoto I., Fukuda Y., et al. Identification of a Novel Gene, GASC1, within an Amplicon at 9p23-24 Frequently Detected in Esophageal Cancer Cell Lines. Cancer Res. 2000 ; 60: 4735-4739
    • (2000) Cancer Res , vol.60 , pp. 4735-4739
    • Yang, Z.Q.1    Imoto, I.2    Fukuda, Y.3
  • 9
    • 72449186524 scopus 로고    scopus 로고
    • Genomic Amplification and Oncogenic Properties of the GASC1 Histone Demethylase Gene in Breast Cancer
    • Liu G., Bollig-Fischer A., Kreike B., et al. Genomic Amplification and Oncogenic Properties of the GASC1 Histone Demethylase Gene in Breast Cancer. Oncogene. 2009 ; 28: 4491-4500
    • (2009) Oncogene , vol.28 , pp. 4491-4500
    • Liu, G.1    Bollig-Fischer, A.2    Kreike, B.3
  • 10
    • 63449115501 scopus 로고    scopus 로고
    • Multiple Recurrent Genetic Events Converge on Control of Histone Lysine Methylation in Medulloblastoma
    • Northcott P. A., Nakahara Y., Wu X., et al. Multiple Recurrent Genetic Events Converge on Control of Histone Lysine Methylation in Medulloblastoma. Nat. Genet. 2009 ; 41: 465-472
    • (2009) Nat. Genet , vol.41 , pp. 465-472
    • Northcott, P.A.1    Nakahara, Y.2    Wu, X.3
  • 11
    • 84866894408 scopus 로고    scopus 로고
    • Comprehensive Genomic Characterization of Squamous Cell Lung Cancers
    • Hammerman P. S., Hayes D. N., Wilkerson M. D., et al. Comprehensive Genomic Characterization of Squamous Cell Lung Cancers. Nature. 2012 ; 489: 519-525
    • (2012) Nature , vol.489 , pp. 519-525
    • Hammerman, P.S.1    Hayes, D.N.2    Wilkerson, M.D.3
  • 12
    • 58149198591 scopus 로고    scopus 로고
    • Mucosa-Associated Lymphoid Tissue Lymphoma: Novel Translocations Including Rearrangements of ODZ2, JMJD2C, and CNN3
    • Vinatzer U., Gollinger M., Mullauer L., et al. Mucosa-Associated Lymphoid Tissue Lymphoma: Novel Translocations Including Rearrangements of ODZ2, JMJD2C, and CNN3. Clin. Cancer Res. 2008 ; 14: 6426-6431
    • (2008) Clin. Cancer Res , vol.14 , pp. 6426-6431
    • Vinatzer, U.1    Gollinger, M.2    Mullauer, L.3
  • 13
    • 33745187327 scopus 로고    scopus 로고
    • Histone H3 Lysine 4 Demethylation is a Target of Nonselective Antidepressive Medications
    • Lee M. G., Wynder C., Schmidt D. M., et al. Histone H3 Lysine 4 Demethylation Is a Target of Nonselective Antidepressive Medications. Chem. Biol. 2006 ; 13: 563-567
    • (2006) Chem. Biol , vol.13 , pp. 563-567
    • Lee, M.G.1    Wynder, C.2    Schmidt, D.M.3
  • 14
    • 56749151276 scopus 로고    scopus 로고
    • Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases
    • Rose N. R., Ng S. S., Mecinovic J., et al. Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases. J. Med. Chem. 2008 ; 51: 7053-7056
    • (2008) J. Med. Chem , vol.51 , pp. 7053-7056
    • Rose, N.R.1    Ng, S.S.2    Mecinovic, J.3
  • 15
    • 79955035374 scopus 로고    scopus 로고
    • Inhibition of Histone Demethylases by 4-Carboxy-2,2′-Bipyridyl Compounds
    • Chang K. H., King O. N., Tumber A., et al. Inhibition of Histone Demethylases by 4-Carboxy-2,2′-Bipyridyl Compounds. ChemMedChem. 2011 ; 6: 759-764
    • (2011) ChemMedChem , vol.6 , pp. 759-764
    • Chang, K.H.1    King, O.N.2    Tumber, A.3
  • 16
    • 33748989795 scopus 로고    scopus 로고
    • Crystal Structure of Human Histone Lysine-Specific Demethylase 1 (LSD1)
    • Chen Y., Yang Y., Wang F., et al. Crystal Structure of Human Histone Lysine-Specific Demethylase 1 (LSD1). Proc. Natl. Acad. Sci. U. S. A. 2006 ; 103: 13956-13961
    • (2006) Proc. Natl. Acad. Sci. U. S. A , vol.103 , pp. 13956-13961
    • Chen, Y.1    Yang, Y.2    Wang, F.3
  • 17
    • 79955547561 scopus 로고    scopus 로고
    • The Oncometabolite 2-Hydroxyglutarate Inhibits Histone Lysine Demethylases
    • Chowdhury R., Yeoh K. K., Tian Y. M., et al. The Oncometabolite 2-Hydroxyglutarate Inhibits Histone Lysine Demethylases. EMBO Rep. 2011 ; 12: 463-469
    • (2011) EMBO Rep , vol.12 , pp. 463-469
    • Chowdhury, R.1    Yeoh, K.K.2    Tian, Y.M.3
  • 18
    • 34548351239 scopus 로고    scopus 로고
    • A Simple Assay for Detection of Small-Molecule Redox Activity
    • Lor L. A., Schneck J., McNulty D. E., et al. A Simple Assay for Detection of Small-Molecule Redox Activity. J. Biomol. Screen. 2007 ; 12: 881-890
    • (2007) J. Biomol. Screen , vol.12 , pp. 881-890
    • Lor, L.A.1    Schneck, J.2    McNulty, D.E.3
  • 19
    • 0033003760 scopus 로고    scopus 로고
    • A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays
    • 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
    • (1999) J. Biomol. Screen , vol.4 , pp. 67-73
    • Zhang, J.H.1    Chung, T.D.2    Oldenburg, K.R.3
  • 20
    • 11144332565 scopus 로고    scopus 로고
    • Histone Demethylation Mediated by the Nuclear Amine Oxidase Homolog LSD1
    • Shi Y., Lan F., Matson C., et al. Histone Demethylation Mediated by the Nuclear Amine Oxidase Homolog LSD1. Cell. 2004 ; 119: 941-953
    • (2004) Cell , vol.119 , pp. 941-953
    • Shi, Y.1    Lan, F.2    Matson, C.3
  • 21
    • 0031054864 scopus 로고    scopus 로고
    • Spectroscopic Properties of Escherichia coli UDP-N-Acetylenolpyruvylglucosamine Reductase
    • Axley M. J., Fairman R., Yanchunas J., et al. Spectroscopic Properties of Escherichia coli UDP-N-Acetylenolpyruvylglucosamine Reductase. Biochemistry. 1997 ; 36: 812-822
    • (1997) Biochemistry , vol.36 , pp. 812-822
    • Axley, M.J.1    Fairman, R.2    Yanchunas, J.3
  • 22
    • 34147173308 scopus 로고    scopus 로고
    • Trans-2-Phenylcyclopropylamine is a Mechanism-Based Inactivator of the Histone Demethylase LSD1
    • Schmidt D. M., McCafferty D. G.. Trans-2-Phenylcyclopropylamine Is a Mechanism-Based Inactivator of the Histone Demethylase LSD1. Biochemistry. 2007 ; 46: 4408-4416
    • (2007) Biochemistry , vol.46 , pp. 4408-4416
    • Schmidt, D.M.1    McCafferty, D.G.2
  • 23
    • 33746332412 scopus 로고    scopus 로고
    • The Putative Oncogene GASC1 Demethylates Tri- and Dimethylated Lysine 9 on Histone H3
    • Cloos P. A., Christensen J., Agger K., et al. The Putative Oncogene GASC1 Demethylates Tri- and Dimethylated Lysine 9 on Histone H3. Nature. 2006 ; 442: 307-311
    • (2006) Nature , vol.442 , pp. 307-311
    • Cloos, P.A.1    Christensen, J.2    Agger, K.3
  • 24
    • 61849124218 scopus 로고    scopus 로고
    • Defining Balanced Conditions for Inhibitor Screening Assays That Target Bisubstrate Enzymes
    • Yang J., Copeland R. A., Lai Z.. Defining Balanced Conditions for Inhibitor Screening Assays That Target Bisubstrate Enzymes. J. Biomol. Screen. 2009 ; 14: 111-120
    • (2009) J. Biomol. Screen , vol.14 , pp. 111-120
    • Yang, J.1    Copeland, R.A.2    Lai, Z.3
  • 25
    • 75749150081 scopus 로고    scopus 로고
    • A Miniaturized Screen for Inhibitors of Jumonji Histone Demethylases
    • Sakurai M., Rose N. R., Schultz L., et al. A Miniaturized Screen for Inhibitors of Jumonji Histone Demethylases. Mol. Biosyst. 2010 ; 6: 357-364
    • (2010) Mol. Biosyst , vol.6 , pp. 357-364
    • Sakurai, M.1    Rose, N.R.2    Schultz, L.3
  • 26
    • 0031573408 scopus 로고    scopus 로고
    • A One-Step Fluorometric Method for the Continuous Measurement of Monoamine Oxidase Activity
    • Zhou M., Panchuk-Voloshina N.. A One-Step Fluorometric Method for the Continuous Measurement of Monoamine Oxidase Activity. Anal. Biochem. 1997 ; 253: 169-174
    • (1997) Anal. Biochem , vol.253 , pp. 169-174
    • Zhou, M.1    Panchuk-Voloshina, N.2
  • 27
    • 77955399089 scopus 로고    scopus 로고
    • Accessing Protein Methyltransferase and Demethylase Enzymology Using Microfluidic Capillary Electrophoresis
    • Wigle T. J., Provencher L. M., Norris J. L., et al. Accessing Protein Methyltransferase and Demethylase Enzymology Using Microfluidic Capillary Electrophoresis. Chem. Biol. 2010 ; 17: 695-704
    • (2010) Chem. Biol , vol.17 , pp. 695-704
    • Wigle, T.J.1    Provencher, L.M.2    Norris, J.L.3
  • 28
    • 84857306199 scopus 로고    scopus 로고
    • High-Throughput TR-FRET Assays for Identifying Inhibitors of LSD1 and JMJD2C Histone Lysine Demethylases
    • Yu V., Fisch T., Long A. M., et al. High-Throughput TR-FRET Assays for Identifying Inhibitors of LSD1 and JMJD2C Histone Lysine Demethylases. J. Biomol. Screen. 2012 ; 17: 27-38
    • (2012) J. Biomol. Screen , vol.17 , pp. 27-38
    • Yu, V.1    Fisch, T.2    Long, A.M.3
  • 29
    • 84859823620 scopus 로고    scopus 로고
    • A Sensitive, Homogeneous, and High-Throughput Assay for Lysine-Specific Histone Demethylases at the H3K4 Site
    • Wang C., Caron M., Burdick D., et al. A Sensitive, Homogeneous, and High-Throughput Assay for Lysine-Specific Histone Demethylases at the H3K4 Site. Assay Drug Dev. Technol. 2012 ; 10: 179-186
    • (2012) Assay Drug Dev. Technol , vol.10 , pp. 179-186
    • Wang, C.1    Caron, M.2    Burdick, D.3
  • 30
    • 80054085409 scopus 로고    scopus 로고
    • Screening for Lysine-Specific Demethylase-1 Inhibitors Using a Label-Free High-Throughput Mass Spectrometry Assay
    • Plant M., Dineen T., Cheng A., et al. Screening for Lysine-Specific Demethylase-1 Inhibitors Using a Label-Free High-Throughput Mass Spectrometry Assay. Anal. Biochem. 2011 ; 419: 217-227
    • (2011) Anal. Biochem , vol.419 , pp. 217-227
    • Plant, M.1    Dineen, T.2    Cheng, A.3
  • 31
    • 84861809953 scopus 로고    scopus 로고
    • Enabling Lead Discovery for Histone Lysine Demethylases by High-Throughput RapidFire Mass Spectrometry
    • Hutchinson S. E., Leveridge M. V., Heathcote M. L., et al. Enabling Lead Discovery for Histone Lysine Demethylases by High-Throughput RapidFire Mass Spectrometry. J. Biomol. Screen. 2012 ; 17: 39-48
    • (2012) J. Biomol. Screen , vol.17 , pp. 39-48
    • Hutchinson, S.E.1    Leveridge, M.V.2    Heathcote, M.L.3
  • 32
    • 84869237494 scopus 로고    scopus 로고
    • Broad Ranges of Affinity and Specificity of Anti-Histone Antibodies Revealed by a Quantitative Peptide Immunoprecipitation Assay
    • Nishikori S., Hattori T., Fuchs S. M., et al. Broad Ranges of Affinity and Specificity of Anti-Histone Antibodies Revealed by a Quantitative Peptide Immunoprecipitation Assay. J. Mol. Biol. 2012 ; 424: 391-399
    • (2012) J. Mol. Biol , vol.424 , pp. 391-399
    • Nishikori, S.1    Hattori, T.2    Fuchs, S.M.3
  • 33
    • 42549116321 scopus 로고    scopus 로고
    • Mass Spectrometry of Self-Assembled Monolayers: A New Tool for Molecular Surface Science
    • Mrksich M.. Mass Spectrometry of Self-Assembled Monolayers: A New Tool for Molecular Surface Science. ACS Nano. 2008 ; 2: 7-18
    • (2008) ACS Nano , vol.2 , pp. 7-18
    • Mrksich, M.1
  • 34
    • 79960233029 scopus 로고    scopus 로고
    • High-Throughput Screening of Small Molecule Libraries Using SAMDI Mass Spectrometry
    • Gurard-Levin Z. A., Scholle M. D., Eisenberg A. H., et al. High-Throughput Screening of Small Molecule Libraries Using SAMDI Mass Spectrometry. ACS Comb. Sci. 2011 ; 13: 347-350
    • (2011) ACS Comb. Sci , vol.13 , pp. 347-350
    • Gurard-Levin, Z.A.1    Scholle, M.D.2    Eisenberg, A.H.3
  • 35
    • 78649528262 scopus 로고    scopus 로고
    • Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors
    • King O. N., Li X. S., Sakurai M., et al. Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors. PLoS One. 2010 ; 5: e15535
    • (2010) PLoS One , vol.5 , pp. 15535
    • King, O.N.1    Li, X.S.2    Sakurai, M.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.