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Cyclic tetrapeptides with –SS– bridging between amino acid side chains for potent histone deacetylases’ inhibition
| Content Provider | Semantic Scholar |
|---|---|
| Author | Arai, Toru Hoque, Ashraful Nishino, Norikazu Kim, Hyonok Ito, Akihiro Yoshida, Minoru |
| Copyright Year | 2013 |
| Abstract | 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. |
| Starting Page | 835 |
| Ending Page | 843 |
| Page Count | 9 |
| File Format | PDF HTM / HTML |
| DOI | 10.1007/s00726-013-1527-8 |
| Alternate Webpage(s) | http://www.riken.jp/SPD/ChemicalGeneticsLab/Jounal/Arai_T2013.pdf |
| PubMed reference number | 23754115 |
| Alternate Webpage(s) | https://doi.org/10.1007/s00726-013-1527-8 |
| Journal | Medline |
| Volume Number | 45 |
| Journal | Amino Acids |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
