4.8 Article

Synthesis and Conformation-Activity Relationships of the Peptide Isosteres of FK228 and Largazole

Journal

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 131, Issue 8, Pages 2900-2905

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ja807772w

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Funding

  1. NCI NIH HHS [K08 CA128972-01A1, K08 CA128972, CA136283, F32 CA136283, 1K08CA128972] Funding Source: Medline
  2. NIGMS NIH HHS [GM49631] Funding Source: Medline
  3. Wellcome Trust Funding Source: Medline

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The peptide isosteres (110 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.

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