Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length.
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.
Islam
Nurul M
NM
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kitakyushu 808-0196, Japan.
Kato
Tamaki
T
Nishino
Norikazu
N
Kim
Hyun-Jung
HJ
Ito
Akihiro
A
Yoshida
Minoru
M
D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D006655:Histone Deacetylases / Q000737:chemistry / Q000378:metabolism*; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology
D001643:Bridged Bicyclo Compounds; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D009842:Oligopeptides; D006655:Histone Deacetylases