1380236-06-5Relevant academic research and scientific papers
Cyclic tetrapeptides with-SS-bridging between amino acid side chains for potent histone deacetylases' inhibition
Arai, Toru,Ashraful Hoque,Nishino, Norikazu,Kim, Hyun-Jung,Ito, Akihiro,Yoshida, Minoru
, p. 835 - 843 (2013)
Cyclic depsipeptide FK228 with an intramolecular disulfide bond is a potent inhibitor of histone deacetylases (HDAC). FK228 is stable in blood because of its prodrug function, whose -SS- bond is reduced within the cell. Here, cyclic peptides with -SS- bridges between a variety of amino acids were synthesized and assayed for HDAC inhibition. Cyclic peptide 3, cyclo(-l-amino acid-l-amino acid-l-Val-d-Pro-), with an -SS- bridge between the first and second amino acids, was found to be a potent HDAC inhibitor. Cyclic peptide 7, cyclo(-l-amino acid-d-amino acid-l-Val-d-Pro-), with an -SS- bridge between the first and second amino acids, was also a potent HDAC inhibitor.
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases
Hoque, Md. Ashraful,Arai, Toru,Nishino, Norikazu,Kim, Hyun-Jung,Ito, Akihiro,Yoshida, Minoru
, p. 6770 - 6772 (2013/01/14)
Two thioacetate tails were introduced to the chlamydocin- and CHAP31-related cyclic tetrapeptides. An intramolecular disulfide bridge could be formed in the CHAP31-related cyclic peptides. Both the thioacetate-tailed and disulfide-bridged peptides were po
