1380236-70-3Relevant academic research and scientific papers
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors
Hoque, Md. Ashraful,Islam, Md. Nurul,Islam, Md. Shahidul,Kato, Tamaki,Nishino, Norikazu,Ito, Akihiro,Yoshida, Minoru
, p. 3850 - 3855 (2014)
The naturally occurring cyclic depsipeptide, FK228 inhibits histone deacetylase (HDAC) enzymes after reductive cleavage of intra-molecular disulfide bond. One of the sulfhydryl groups produced in the reduction interacts with zinc atom that involved in the
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 (2013/10/22)
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.
