NDLI: Evaluation of functional groups on amino acids in cyclic tetrapeptides in histone deacetylase inhibition

Content Provider	Springer Nature Link
Author	Islam, Md. Shahidul Bhuiyan, Mohammed P. I. Islam, Md. Nurul Nsiama, Tienabe Kipassa Oishi, Naoto Kato, Tamaki Nishi, rikazu Ito, Akihiro Yoshida, Miru
Copyright Year	2011
Abstract	The naturally occurring cyclic tetrapeptide, chlamydocin, originally isolated from fungus Diheterospora chlamydosphoria, consists of α-aminoisobutyric acid, l-phenylalanine, d-proline and an unusual amino acid (S)-2-amino-8-((S)-oxiran-2-yl)-8-oxooctanoic acid (Aoe) and inhibits the histone deacetylases (HDACs), a class of regulatory enzymes. The epoxyketone moiety of Aoe is the key functional group for inhibition. The cyclic tetrapeptide scaffold is supposed to play important role for effective binding to the surface of enzymes. In place of the epoxyketone group, hydroxamic acid and sulfhydryl group have been applied to design inhibitor ligands to zinc atom in catalytic site of HDACs. In the research for more potent HDAC inhibitors, we replaced the epoxyketone moiety of Aoe with different functional groups and synthesized a series of chlamydocin analogs as HDAC inhibitors. Among the functional groups, methoxymethylketone moiety showed as potent inhibition as the hydroxamic acid. On the contrary, we confirmed that borate, trifruoromethylketone, and 2-aminoanilide are almost inactive in HDAC inhibition.
Starting Page	2103
Ending Page	2110
Page Count	8
File Format	PDF
ISSN	09394451
Journal	Amino Acids
Volume Number	42
Issue Number	6
e-ISSN	14382199
Language	English
Publisher	Springer Vienna
Publisher Date	2011-06-03
Publisher Place	Vienna
Access Restriction	Subscribed
Subject Keyword	Histone deacetylase inhibitor Chlamydocin Epoxyketone Functional group design Biochemical Engineering Analytical Chemistry Biochemistry Proteomics Life Sciences Neurobiology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Biochemistry Clinical Biochemistry

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