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Literature DB >> 23725560

Quantitative analysis of histone demethylase probes using fluorescence polarization.

Wenqing Xu¹, Jessica D Podoll, Xuan Dong, Anthony Tumber, Udo Oppermann, Xiang Wang.

Abstract

We previously reported methylstat as a selective inhibitor of jumonji C domain-containing histone demethylases (JHDMs). Herein, we describe the synthesis of a fluorescent analogue of methylstat and its application as a tracer in fluorescence polarization assays. Using this format, we have evaluated the binding affinities of several known JHDM probes, as well as the native cofactor and substrate of JHDM1A. This fluorophore allowed a highly robust and miniaturized competition assay sufficient for high-throughput screening.

Entities: Chemical Disease Gene Species

Mesh：

Substances：

Year: 2013 PMID： 23725560 PMCID： PMC3724763 DOI： 10.1021/jm3018628

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

22 in total

1. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays.

Authors:
Journal: J Biomol Screen Date: 1999

2. Fluorescence polarization competition assay: the range of resolvable inhibitor potency is limited by the affinity of the fluorescent ligand.

Authors: Xinyi Huang
Journal: J Biomol Screen Date: 2003-02

Review 3. Histone demethylases in development and disease.

Authors: Marianne Terndrup Pedersen; Kristian Helin
Journal: Trends Cell Biol Date: 2010-09-20 Impact factor: 20.808

4. 2-Oxoglutarate oxygenases are inhibited by a range of transition metals.

Authors: Rok Sekirnik; Nathan R Rose; Jasmin Mecinović; Christopher J Schofield
Journal: Metallomics Date: 2010-05-20 Impact factor: 4.526

5. A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.

Authors: Xuelai Luo; Yongxiang Liu; Stefan Kubicek; Johanna Myllyharju; Anthony Tumber; Stanley Ng; Ka Hing Che; Jessica Podoll; Tom D Heightman; Udo Oppermann; Stuart L Schreiber; Xiang Wang
Journal: J Am Chem Soc Date: 2011-05-31 Impact factor: 15.419

6. Crystal structures of histone demethylase JMJD2A reveal basis for substrate specificity.

Authors: Stanley S Ng; Kathryn L Kavanagh; Michael A McDonough; Danica Butler; Ewa S Pilka; Benoit M R Lienard; James E Bray; Pavel Savitsky; Opher Gileadi; Frank von Delft; Nathan R Rose; John Offer; Johanna C Scheinost; Tomasz Borowski; Michael Sundstrom; Christopher J Schofield; Udo Oppermann
Journal: Nature Date: 2007-06-24 Impact factor: 49.962

7. Specificity and mechanism of JMJD2A, a trimethyllysine-specific histone demethylase.

Authors: Jean-François Couture; Evys Collazo; Patricia A Ortiz-Tello; Joseph S Brunzelle; Raymond C Trievel
Journal: Nat Struct Mol Biol Date: 2007-06-24 Impact factor: 15.369

8. Analysis of protein-ligand interactions by fluorescence polarization.

Authors: Ana M Rossi; Colin W Taylor
Journal: Nat Protoc Date: 2011-03-03 Impact factor: 13.491

9. Linking of 2-oxoglutarate and substrate binding sites enables potent and highly selective inhibition of JmjC histone demethylases.

Authors: Esther C Y Woon; Anthony Tumber; Akane Kawamura; Lars Hillringhaus; Wei Ge; Nathan R Rose; Jerome H Y Ma; Mun Chiang Chan; Louise J Walport; Ka Hing Che; Stanley S Ng; Brian D Marsden; Udo Oppermann; Michael A McDonough; Christopher J Schofield
Journal: Angew Chem Int Ed Engl Date: 2012-01-12 Impact factor: 15.336

10. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.

Authors: Laurens Kruidenier; Chun-wa Chung; Zhongjun Cheng; John Liddle; KaHing Che; Gerard Joberty; Marcus Bantscheff; Chas Bountra; Angela Bridges; Hawa Diallo; Dirk Eberhard; Sue Hutchinson; Emma Jones; Roy Katso; Melanie Leveridge; Palwinder K Mander; Julie Mosley; Cesar Ramirez-Molina; Paul Rowland; Christopher J Schofield; Robert J Sheppard; Julia E Smith; Catherine Swales; Robert Tanner; Pamela Thomas; Anthony Tumber; Gerard Drewes; Udo Oppermann; Dinshaw J Patel; Kevin Lee; David M Wilson
Journal: Nature Date: 2012-08-16 Impact factor: 49.962

7 in total

Quantitative analysis of histone demethylase probes using fluorescence polarization.

1. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays.

2. Fluorescence polarization competition assay: the range of resolvable inhibitor potency is limited by the affinity of the fluorescent ligand.

Review 3. Histone demethylases in development and disease.

4. 2-Oxoglutarate oxygenases are inhibited by a range of transition metals.

5. A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.

6. Crystal structures of histone demethylase JMJD2A reveal basis for substrate specificity.

7. Specificity and mechanism of JMJD2A, a trimethyllysine-specific histone demethylase.

8. Analysis of protein-ligand interactions by fluorescence polarization.

9. Linking of 2-oxoglutarate and substrate binding sites enables potent and highly selective inhibition of JmjC histone demethylases.

10. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.

Review 1. Inhibitors of Protein Methyltransferases and Demethylases.

Review 2. Recent Advances with KDM4 Inhibitors and Potential Applications.

3. Development of substrate-selective probes for affinity pulldown of histone demethylases.

4. Novel Scaffolds of Cell-Active Histone Demethylase Inhibitors Identified from High-Throughput Screening.

Review 5. Digging deep into "dirty" drugs - modulation of the methylation machinery.

6. A Fluorescence Polarization Biophysical Assay for the Naegleria DNA Hydroxylase Tet1.

7. Small molecule KDM4s inhibitors as anti-cancer agents.