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Bioorg Med Chem Lett DOI:10.1016/j.bmcl.2008.04.007

Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.

Publication TypeJournal Article
Year of Publication2008
AuthorsMazitschek, R, Patel, V, Wirth, DF, Clardy, J
JournalBioorg Med Chem Lett
Date Published2008 May 01
KeywordsBiological Assay, Drug Evaluation, Preclinical, Enzyme Inhibitors, Fluorescence Resonance Energy Transfer, Fluorescent Dyes, Histone Deacetylase Inhibitors, Ligands, Substrate Specificity

Histone deacetylases (HDACs) regulate many important physiological processes and the discovery of small molecules that modulate HDAC activity has both academic and clinical relevance. HDAC inhibitors, most notably SAHA, have been pursued as cancer chemotherapeutics but may be useful in treating psychiatric disorders, malaria, and other diseases. Herein, we describe an inexpensive and robust assay, based on fluorescence polarization, for HDAC ligand discovery. The assay is well suited for high-throughput screening and enzyme kinetic studies.


Alternate JournalBioorg. Med. Chem. Lett.
PubMed ID18430569
PubMed Central IDPMC2408937
Grant ListR01 CA059021 / CA / NCI NIH HHS / United States
R01 CA024487 / CA / NCI NIH HHS / United States
R21 NS059404 / NS / NINDS NIH HHS / United States
R01 CA059021-15 / CA / NCI NIH HHS / United States
P01 CA078048 / CA / NCI NIH HHS / United States
R21 NS059404-01 / NS / NINDS NIH HHS / United States
CA24487 / CA / NCI NIH HHS / United States