Synthesis and conformation-activity relationships of the peptide isosteres of FK228 and largazole.

J Am Chem Soc

Authors	Albert Bowers Thomas Greshock Nathan West Guillermina Estiu Stuart Schreiber Olaf Wiest Robert Williams James Bradner
Keywords	Humans Models, Molecular Catalytic Domain Structure-Activity Relationship Thermodynamics Lactams, Macrocyclic Histone Deacetylase 1 Histone Deacetylase Inhibitors Thiazoles Isomerism Depsipeptides
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.
Year of Publication	2009
Journal	J Am Chem Soc
Volume	131
Issue	8
Pages	2900-5
Date Published	2009 Mar 04
ISSN	1520-5126
DOI	10.1021/ja807772w
PubMed ID	19193120
PubMed Central ID	PMC2880701
Links
Grant list	CA136283 / CA / NCI NIH HHS / United States GM49631 / GM / NIGMS NIH HHS / United States K08 CA128972-01A1 / CA / NCI NIH HHS / United States 1K08CA128972 / CA / NCI NIH HHS / United States F32 CA136283 / CA / NCI NIH HHS / United States K08 CA128972 / CA / NCI NIH HHS / United States

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