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CHAPTER 4

Macrocyclic Inhibitors of Zinc-dependent Histone Deacetylases (HDACs)

The modulation of epigenetic targets has recently become an attractive strategy for drug discovery. Among these, it is the inhibition of histone deacetylases (HDACs) that has received the most attention. Numerous HDAC inhibitors have advanced to clinical trials and two have received FDA approval as anticancer agents. This chapter reviews natural and synthetic inhibitors of zinc-dependent HDACs that contain a macrocyclic scaffold including the trapoxin and apicidin cyclic tetrapeptides, the FK228 depsipeptide family, the azumamides and fully synthetic macrocycles.

Publication details


Print publication date
16 Oct 2014
Copyright year
2015
Print ISBN
978-1-84973-701-2
PDF eISBN
978-1-78262-311-3
ePub eISBN
978-1-78262-316-8
From the book series:
Drug Discovery