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

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.

SUBMITTER: Bowers AA

PROVIDER: S-EPMC2880701 | biostudies-literature | 2009 Mar

REPOSITORIES: biostudies-literature

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

Bowers Albert A AA Greshock Thomas J TJ West Nathan N Estiu Guillermina G Schreiber Stuart L SL Wiest Olaf O Williams Robert M RM Bradner James E JE

Journal of the American Chemical Society 20090301 8

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. ...[more]

PMID: 19193120

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