Document Detail


Hexylitaconic acid: a new inhibitor of p53-HDM2 interaction isolated from a marine-derived fungus, Arthrinium sp.
MedLine Citation:
PMID:  16246554     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A new inhibitor of p53-HDM2 interaction was isolated from a culture of marine-derived fungus, Arthrinium sp. The structure was identified to be (-)-hexylitaconic acid (1) by spectroscopic analysis. The inhibition of p53-HDM2 binding was tested by the ELISA method, and 1 inhibited the binding with an IC(50) value of 50 microg/mL. Although a number of synthetic inhibitors of p53-HDM2 interaction have been reported so far, 1 is the second inhibitor isolated from natural resources.
Authors:
Sachiko Tsukamoto; Takushi Yoshida; Hidetaka Hosono; Tomihisa Ohta; Hideyoshi Yokosawa
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2005-10-21
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  16     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2006 Jan 
Date Detail:
Created Date:  2005-11-18     Completed Date:  2006-03-21     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  69-71     Citation Subset:  IM    
Affiliation:
Graduate School of Natural Science and Technology, Kanazawa University, Kanazawa 920-1192, Japan. sachiko@p.kanazawa-u.ac.jp
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MeSH Terms
Descriptor/Qualifier:
Ascomycota / metabolism*
Chemistry, Pharmaceutical / methods*
Crystallography, X-Ray
Dose-Response Relationship, Drug
Drug Design*
Enzyme Inhibitors / pharmacology*
Enzyme-Linked Immunosorbent Assay
Fungal Proteins / chemistry
Humans
Inhibitory Concentration 50
Models, Chemical
Protein Binding
Proto-Oncogene Proteins c-mdm2 / metabolism*
Succinates / chemistry*
Tumor Suppressor Protein p53 / chemistry*,  metabolism
Chemical
Reg. No./Substance:
0/2-methylene-3-hexylbutanedioic acid; 0/Enzyme Inhibitors; 0/Fungal Proteins; 0/Succinates; 0/Tumor Suppressor Protein p53; EC 6.3.2.19/MDM2 protein, human; EC 6.3.2.19/Proto-Oncogene Proteins c-mdm2

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


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