Document Detail


FR182876, a new microtubule modulator with high water-solubility, from a Streptomyces.
MedLine Citation:
PMID:  15376555     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In the course of seeking new anti-tumor drugs, a new microtubule modulator with high water-solubility, FR182876, was isolated from a Streptomyces which also produces FR182877. Even modern spectroscopic methods could not solve the structure of FR182876 due to its structural complexity and chemical instability. Thus, we have combined chemical correlations with spectroscopic methods and determined its structure, which features a highly fused ring system and 3-methylhistidine. The latter is believed to contribute to both solubility in water and activity in promoting tubulin polymerization. FR182876 showed potent cytotoxicity against a panel of cancer cells at concentrations of 28-75 ng/ml.
Authors:
Seiji Yoshimura; Bunji Sato; Shigehiro Takase; Hiroshi Terano
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Journal of antibiotics     Volume:  57     ISSN:  0021-8820     ISO Abbreviation:  J. Antibiot.     Publication Date:  2004 Jul 
Date Detail:
Created Date:  2004-09-20     Completed Date:  2004-10-13     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0151115     Medline TA:  J Antibiot (Tokyo)     Country:  Japan    
Other Details:
Languages:  eng     Pagination:  429-35     Citation Subset:  IM    
Affiliation:
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 5-2-3, Tokodai, Tsukuba 300-2698, Japan. seiji_yoshimura@po.fujisawa.co.jp
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MeSH Terms
Descriptor/Qualifier:
Antibiotics, Antineoplastic / chemistry,  isolation & purification*,  pharmacology
Cell Line, Tumor
Heterocyclic Compounds with 4 or More Rings / chemistry,  isolation & purification*,  pharmacology
Humans
Microtubules / drug effects*
Solubility
Streptomyces / metabolism*
Chemical
Reg. No./Substance:
0/Antibiotics, Antineoplastic; 0/FR 182876; 0/Heterocyclic Compounds with 4 or More Rings

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


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