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Drug Discovery
Macrocycles in Drug Discovery
Edited by
Jeremy Levin
Jeremy Levin
Boehringer Ingelheim, USA
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Hardback ISBN:
978-1-84973-701-2
PDF ISBN:
978-1-78262-311-3
EPUB ISBN:
978-1-78262-316-8
Special Collection:
2014 ebook collection
,
2011-2015 industrial and pharmaceutical chemistry subject collection
Series:
Drug Discovery
No. of Pages:
528
Published online:
03 Oct 2014
Published in print:
16 Oct 2014
Book Chapter
CHAPTER 4: Macrocyclic Inhibitors of Zinc-dependent Histone Deacetylases (HDACs)
By
A. Ganesan
A. Ganesan
School of Pharmacy, University of East Anglia
Norwich Research Park
Norwich NR4 7TJ
UK
[email protected]
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Published:03 Oct 2014
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Special Collection: 2014 ebook collection , 2011-2015 industrial and pharmaceutical chemistry subject collectionSeries: Drug Discovery
Page range:
109 - 140
Citation
A. Ganesan, in Macrocycles in Drug Discovery, ed. J. Levin, The Royal Society of Chemistry, 2014, pp. 109-140.
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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.
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