Cyclic tetrapeptides bearing a sulfhydryl group potently inhibit histone deacetylases.
New inhibitors of histone deacetylase (HDAC) containing a sulfhydryl group were designed on the basis of the corresponding hydroxamic acid (CHAP31) and FK228. Their disulfide dimers and hybrids exhibited potent HDAC inhibitory activity in vivo with potential as anticancer prodrugs. [structure: see text]
Nishino
Norikazu
N
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Hibikino, Wakamatsu-ku, Kitakyushu 808-0196, Japan. nishino@life.kyutech.ac.jp
Jose
Binoy
B
Okamura
Shinji
S
Ebisusaki
Shutoku
S
Kato
Tamaki
T
Sumida
Yuko
Y
Yoshida
Minoru
M
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D003460:Crystallization; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D056572:Histone Deacetylase Inhibitors; D009842:Oligopeptides / Q000737:chemistry / Q000494:pharmacology*; D011355:Prodrugs / Q000737:chemistry / Q000494:pharmacology; D013438:Sulfhydryl Compounds / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D009842:Oligopeptides; D011355:Prodrugs; D013438:Sulfhydryl Compounds