Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length

Nurul M Islam; Tamaki Kato; Norikazu Nishino; Hyun-Jung Kim; Akihiro Ito; Minoru Yoshida

doi:10.1016/j.bmcl.2009.12.054

Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length

Bioorg Med Chem Lett. 2010 Feb 1;20(3):997-9. doi: 10.1016/j.bmcl.2009.12.054. Epub 2009 Dec 21.

Authors

Nurul M Islam¹, Tamaki Kato, Norikazu Nishino, Hyun-Jung Kim, Akihiro Ito, Minoru Yoshida

Affiliation

¹ Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kitakyushu 808-0196, Japan.

PMID: 20045316
DOI: 10.1016/j.bmcl.2009.12.054

Abstract

Bicyclic tetrapeptide hydroxamic acids were prepared as histone deacetylase (HDAC) inhibitors, and the evaluated inhibitory activity shows that they are potent against HDAC1 and HDAC4. The in vivo activity depends on alkyl loop length.

Publication types

Comparative Study

MeSH terms

Bridged Bicyclo Compounds / chemical synthesis
Bridged Bicyclo Compounds / metabolism
Bridged Bicyclo Compounds / pharmacology
Histone Deacetylase Inhibitors / chemical synthesis*
Histone Deacetylase Inhibitors / metabolism
Histone Deacetylase Inhibitors / pharmacology
Histone Deacetylases / chemistry
Histone Deacetylases / metabolism*
Hydroxamic Acids / chemical synthesis*
Hydroxamic Acids / metabolism
Hydroxamic Acids / pharmacology
Oligopeptides / chemical synthesis*
Oligopeptides / metabolism
Oligopeptides / pharmacology

Substances

Bridged Bicyclo Compounds
Histone Deacetylase Inhibitors
Hydroxamic Acids
Oligopeptides
Histone Deacetylases