Communication

Fluorous-Based Small-Molecule Microarrays for the Discovery of Histone Deacetylase Inhibitors†

  1. Arturo J. Vegas1,
  2. James E. Bradner Dr.1,
  3. Weiping Tang Prof. Dr.2,
  4. Olivia M. McPherson1,
  5. Edward F. Greenberg1,
  6. Angela N. Koehler Dr.1,
  7. Stuart L. Schreiber Prof. Dr.1

Article first published online: 17 SEP 2007

DOI: 10.1002/anie.200703198

Issue

Angewandte Chemie International Edition

Angewandte Chemie International Edition

Volume 46, Issue 42, pages 7960–7964, October 22, 2007

Additional Information

How to Cite

Vegas, Arturo J., Bradner, James E., Tang, W., McPherson, Olivia M., Greenberg, Edward F., Koehler, Angela N. and Schreiber, Stuart L. (2007), Fluorous-Based Small-Molecule Microarrays for the Discovery of Histone Deacetylase Inhibitors. Angew. Chem. Int. Ed., 46: 7960–7964. doi: 10.1002/anie.200703198

Author Information

  1. 1

    Howard Hughes Medical Institute, Chemistry and Chemical Biology, Harvard University, Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, MA 02142, USA, Fax: (+1) 617-324-9601 http://www.broad.harvard.edu/chembio

  2. 2

    School of Pharmacy, University of Wisconsin, 777 Highland Avenue, Madison, WI 53705, USA

  1. †

    We would like to thank Dr. Kara Herlihy, Dr. Ralph Mazitschek, Dr. Carlos Tassa, Jason Fuller, Dr. Steve Haggarty, Dr. Jianping Cui, Dr. Letian Kuai, Dr. Marvin Yu, and Dr. Philip Yeske (Fluorous Technologies) for reagents or comments. Work described herein has been funded in whole or in part with Federal funds from the National Cancer Institute's Initiative for Chemical Genetics, National Institutes of Health, under contract no. N01-CO-12400.

Publication History

  1. Issue published online: 12 OCT 2007
  2. Article first published online: 17 SEP 2007
  3. Manuscript Received: 17 JUL 2007

Funded by

  • National Cancer Institute's Initiative for Chemical Genetics
  • National Institutes of Health. Grant Number: N01-CO-12400

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Keywords:

  • chromatin;
  • fluorous tags;
  • high-throughput screening;
  • microarrays
Thumbnail image of graphical abstract

Noncovalent immobilization is an attractive method for identifying inhibitors of histone deacetylases (HDACs). Fluorous-based small-molecule microarrays were validated as an effective method. Three enzymes and three assays (microarray, biochemical activity, and surface plasmon resonance) were used to identify inhibitors of HDACs and to compare them.

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