Synthesis and Conformation−Activity Relationships of the Peptide Isosteres of FK228 and Largazole
- 4 February 2009
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of the American Chemical Society
- Vol. 131 (8), 2900-2905
- https://doi.org/10.1021/ja807772w
Abstract
The peptide isosteres (10 and 11) of the naturally occurring and potent histone deacetylase (HDAC) inhibitors FK228 and largazole have been synthesized and evaluated side-by-side with FK228, largazole, and SAHA for inhibition of the class I HDACs 1, 2, 3, and 6.Keywords
This publication has 55 references indexed in Scilit:
- Optimization of a series of potent and selective ketone histone deacetylase inhibitorsBioorganic & Medicinal Chemistry Letters, 2008
- Residues in the 11 Å Channel of Histone Deacetylase 1 Promote Catalytic Activity: Implications for Designing Isoform-Selective Histone Deacetylase InhibitorsJournal of Medicinal Chemistry, 2008
- Enantioselective Total Synthesis of (+)-Largazole, a Potent Inhibitor of Histone DeacetylaseOrganic Letters, 2008
- Total Synthesis and Biological Mode of Action of Largazole: A Potent Class I Histone Deacetylase InhibitorJournal of the American Chemical Society, 2008
- A Concise Total Synthesis of Largazole, Solution Structure, and Some Preliminary Structure Activity RelationshipsOrganic Letters, 2008
- Improved Total Synthesis of the Potent HDAC Inhibitor FK228 (FR-901228)Organic Letters, 2008
- Fluorous‐Based Small‐Molecule Microarrays for the Discovery of Histone Deacetylase InhibitorsAngewandte Chemie-International Edition, 2007
- Total Synthesis of Azumamides A and EAngewandte Chemie-International Edition, 2006
- Inflammatory subtypes in asthma: Assessment and identification using induced sputumRespirology, 2006
- Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancerNature Reviews Cancer, 2006