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rdf:type |
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lifeskim:mentions |
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0023621,
umls-concept:C0041485,
umls-concept:C0076353,
umls-concept:C0205234,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243077,
umls-concept:C1149960,
umls-concept:C1333258,
umls-concept:C1413258,
umls-concept:C1707627,
umls-concept:C1883254
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pubmed:issue |
20
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pubmed:dateCreated |
2001-9-20
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pubmed:abstractText |
Selective inhibitors of protein tyrosine phosphatases (PTPs) and dual-specificity phosphatases (DSPs) are expected to be useful tools for clarifying the biological functions of the PTPs themselves and also to be candidates for novel therapeutics. We planned a library approach for the identification of PTP/DSP inhibitors in which 3-acyltetronic acid is used as a "core" phosphate mimic. A series of novel tetronic acid derivatives were synthesized and evaluated as inhibitors of the dual-specificity protein phosphatases VHR and cdc25B. Several compounds are found to be potent inhibitors of cdc25B, which is a key enzyme for cell-cycle progression. The promising results described herein strongly indicated that this tetronic acid library is potent as a library focused on the PTP/DSP-selective inhibitor.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
27
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pubmed:volume |
44
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3216-22
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:11563920-Cell Cycle Proteins,
pubmed-meshheading:11563920-Combinatorial Chemistry Techniques,
pubmed-meshheading:11563920-Dual Specificity Phosphatase 3,
pubmed-meshheading:11563920-Enzyme Inhibitors,
pubmed-meshheading:11563920-Escherichia coli,
pubmed-meshheading:11563920-Furans,
pubmed-meshheading:11563920-Models, Molecular,
pubmed-meshheading:11563920-Protein Binding,
pubmed-meshheading:11563920-Protein Tyrosine Phosphatases,
pubmed-meshheading:11563920-Structure-Activity Relationship,
pubmed-meshheading:11563920-cdc25 Phosphatases
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pubmed:year |
2001
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pubmed:articleTitle |
Synthesis of a tetronic acid library focused on inhibitors of tyrosine and dual-specificity protein phosphatases and its evaluation regarding VHR and cdc25B inhibition.
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pubmed:affiliation |
Institute of Multidisciplinary Research for Advanced Materials, Tohoku University, 2-1-1 Katahira, Aoba, Sendai 980-8577, Japan. sodeoka@tagen.tohoku.ac.jp
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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