1009637-48-2Relevant academic research and scientific papers
Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides
Nishino, Norikazu,Shivashimpi, Gururaj M.,Soni, Preeti B.,Bhuiyan, Mohammed P.I.,Kato, Tamaki,Maeda, Satoko,Nishino, Tomonori G.,Yoshida, Minoru
, p. 437 - 445 (2008/09/16)
Inhibitors of histone deacetylases (HDACs) are a promising class of anticancer agents that effect gene regulation. To know the interaction of aliphatic cap groups with HDACs, cyclic tetrapeptide and bicyclic peptide disulfide hybrids were synthesized without aromatic ring in their macrocyclic framework. Benzene ring of l-Phe in chlamydocin was replaced with several aliphatic amino acids and also a fused bicyclic tetrapeptide was synthesized by ring closing metathesis using Grubb's first generation catalyst. The inhibitory activities of the cyclic peptides against histone deacetylase enzymes were evaluated, which demonstrated most of them are interesting candidates as anticancer agents.
Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework
Shivashimpi, Gururaj M.,Amagai, Satoshi,Kato, Tamaki,Nishino, Norikazu,Maeda, Satoko,Nishino, Tomonori G.,Yoshida, Minoru
, p. 7830 - 7839 (2008/09/16)
Chlamydocin, a cyclic tetrapeptide containing aminoisobutyric acid (Aib), l-phenylalanine (l-Phe), d-proline (d-Pro), and a unique amino acid l-2-amino-8-oxo-9,10-epoxydecanoic acid, inhibits the histone deacetylases (HDACs), a class of enzymes, which pla
