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


  • 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.


original image

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.