Document Detail


Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides.
MedLine Citation:
PMID:  17900911     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Norikazu Nishino; Gururaj M Shivashimpi; Preeti B Soni; Mohammed P I Bhuiyan; Tamaki Kato; Satoko Maeda; Tomonori G Nishino; Minoru Yoshida
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2007-09-15
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  16     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2008 Jan 
Date Detail:
Created Date:  2008-01-14     Completed Date:  2008-01-29     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  437-45     Citation Subset:  IM    
Affiliation:
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kitakyushu 808-0196, Japan. nishino@life.kyutech.ac.jp
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents / chemical synthesis
Cell Line
Enzyme Inhibitors / chemical synthesis,  pharmacology
Histone Deacetylase 1
Histone Deacetylase Inhibitors*
Humans
Inhibitory Concentration 50
Peptides, Cyclic / chemical synthesis*,  pharmacology*
Repressor Proteins
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Enzyme Inhibitors; 0/Histone Deacetylase Inhibitors; 0/Peptides, Cyclic; 0/Repressor Proteins; EC 3.5.1.98/HDAC1 protein, human; EC 3.5.1.98/HDAC4 protein, human; EC 3.5.1.98/HDAC6 protein, human; EC 3.5.1.98/Histone Deacetylase 1

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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