Contents
Targeting the Zinc-Dependent Histone Deacetylases (HDACs)
for Drug Discovery . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .
1
A. Ganesan
Hydroxamic Acid-Containing Peptides in the Study of Histone
Deacetylases . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 29
Carlos Moreno-Yruela and Christian A. Olsen
Sirtuin Inhibitors and Activators . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 55
Minna Rahnasto-Rilla, Jonna Tyni, and Maija Lahtela-Kakkonen
Histone Acetyltransferase Enzymes: From Biological Implications
to Most Relevant Inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 93
Daniela Trisciuoglio and Dante Rotili
Lysine Methyltransferases and Their Inhibitors . . . . . . . . . . . . . . . . . . . 123
Giulia Stazi, Clemens Zwergel, and Sergio Valente
PRMT Inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 159
Matthijs J. van Haren and Nathaniel I. Martin
Lysine-Specific Histone Demethylases 1/2 (LSD1/2) and
Their Inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 197
Takayoshi Suzuki
Inhibitors of JmjC-Containing Histone Demethylases . . . . . . . . . . . . . . . 221
Miranda Wright, Paul E. Brennan, and Akane Kawamura
Chemical Compounds Targeting DNA Methylation and
Hydroxymethylation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 255
Roman Belle, Akane Kawamura, and Paola B. Arimondo
Applied Biophysics for Bromodomain Drug Discovery . . . . . . . . . . . . . . 287
William C. K. Pomerantz, Jorden A. Johnson, and Peter D. Ycas
vii