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Evaluation of class I HDAC isoform selectivity of largazole analogues.

Publication ,  Journal Article
Kim, B; Park, H; Salvador, LA; Serrano, PE; Kwan, JC; Zeller, SL; Chen, Q-Y; Ryu, S; Liu, Y; Byeon, S; Luesch, H; Hong, J
Published in: Bioorganic & medicinal chemistry letters
August 2014

Largazole is a potent class I selective histone deacetylase (HDAC) inhibitor. The majority of largazole analogues to date have modified the thiazole-thiazoline and the warhead moiety. In order to elucidate class I-specific structure-activity relationships, a series of analogues with modifications in the valine or the linker region were prepared and evaluated for their class I isoform selectivity. The inhibition profile showed that the C2 position of largazole has an optimal steric requirement for efficient HDAC inhibition and that substitution of the trans-alkene in the linker with an aromatic group results in complete loss of activity. This data will aid the design of class I isoform selective HDAC inhibitors.

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Published In

Bioorganic & medicinal chemistry letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

August 2014

Volume

24

Issue

16

Start / End Page

3728 / 3731

Related Subject Headings

  • Thiazoles
  • Structure-Activity Relationship
  • Molecular Structure
  • Medicinal & Biomolecular Chemistry
  • Isoenzymes
  • Humans
  • Histone Deacetylase Inhibitors
  • Histone Deacetylase 1
  • Dose-Response Relationship, Drug
  • Depsipeptides
 

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Kim, B., Park, H., Salvador, L. A., Serrano, P. E., Kwan, J. C., Zeller, S. L., … Hong, J. (2014). Evaluation of class I HDAC isoform selectivity of largazole analogues. Bioorganic & Medicinal Chemistry Letters, 24(16), 3728–3731. https://doi.org/10.1016/j.bmcl.2014.07.006
Kim, Bumki, Heekwang Park, Lilibeth A. Salvador, Patrick E. Serrano, Jason C. Kwan, Sabrina L. Zeller, Qi-Yin Chen, et al. “Evaluation of class I HDAC isoform selectivity of largazole analogues.Bioorganic & Medicinal Chemistry Letters 24, no. 16 (August 2014): 3728–31. https://doi.org/10.1016/j.bmcl.2014.07.006.
Kim B, Park H, Salvador LA, Serrano PE, Kwan JC, Zeller SL, et al. Evaluation of class I HDAC isoform selectivity of largazole analogues. Bioorganic & medicinal chemistry letters. 2014 Aug;24(16):3728–31.
Kim, Bumki, et al. “Evaluation of class I HDAC isoform selectivity of largazole analogues.Bioorganic & Medicinal Chemistry Letters, vol. 24, no. 16, Aug. 2014, pp. 3728–31. Epmc, doi:10.1016/j.bmcl.2014.07.006.
Kim B, Park H, Salvador LA, Serrano PE, Kwan JC, Zeller SL, Chen Q-Y, Ryu S, Liu Y, Byeon S, Luesch H, Hong J. Evaluation of class I HDAC isoform selectivity of largazole analogues. Bioorganic & medicinal chemistry letters. 2014 Aug;24(16):3728–3731.
Journal cover image

Published In

Bioorganic & medicinal chemistry letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

August 2014

Volume

24

Issue

16

Start / End Page

3728 / 3731

Related Subject Headings

  • Thiazoles
  • Structure-Activity Relationship
  • Molecular Structure
  • Medicinal & Biomolecular Chemistry
  • Isoenzymes
  • Humans
  • Histone Deacetylase Inhibitors
  • Histone Deacetylase 1
  • Dose-Response Relationship, Drug
  • Depsipeptides