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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2002-6-6
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pubmed:abstractText |
Peptidic Mouse Double Minute (MDM2) inhibitors have been demonstrated to effectively inhibit the interaction between p53 and MDM2, thus providing a therapeutic strategy for some tumors. However, there is no report on non-peptidic inhibitors. In this study non-peptidic HDM2 (the human homologue of MDM2) inhibitors were obtained by computer-aided design and subsequently synthesized by chemical method. Bio-evaluation showed that some of these inhibitors have affinity with HDM2, and can cause death of some tumor cells which express wild-type p53. Cellular assays showed that one of these compounds, syc-7, can activate the p53 pathway in some of these tumor cell lines, and further induce apoptosis. The results suggest that developing non-peptidic small-molecule HDM2 inhibitors is a promising way for new antitumor drug discovery.
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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 |
0304-3835
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
8
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pubmed:volume |
183
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
69-77
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12049816-Antineoplastic Agents,
pubmed-meshheading:12049816-Apoptosis,
pubmed-meshheading:12049816-Breast Neoplasms,
pubmed-meshheading:12049816-Carcinoma, Small Cell,
pubmed-meshheading:12049816-Cell Survival,
pubmed-meshheading:12049816-Enzyme-Linked Immunosorbent Assay,
pubmed-meshheading:12049816-Female,
pubmed-meshheading:12049816-HeLa Cells,
pubmed-meshheading:12049816-Humans,
pubmed-meshheading:12049816-Lung Neoplasms,
pubmed-meshheading:12049816-Neoplasm Proteins,
pubmed-meshheading:12049816-Nuclear Proteins,
pubmed-meshheading:12049816-Proto-Oncogene Proteins,
pubmed-meshheading:12049816-Proto-Oncogene Proteins c-mdm2,
pubmed-meshheading:12049816-Structure-Activity Relationship,
pubmed-meshheading:12049816-Tumor Cells, Cultured,
pubmed-meshheading:12049816-Tumor Suppressor Protein p53
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pubmed:year |
2002
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pubmed:articleTitle |
The initial evaluation of non-peptidic small-molecule HDM2 inhibitors based on p53-HDM2 complex structure.
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pubmed:affiliation |
National Laboratory of Molecular Oncology, Cancer Institute, Peking Union Medical College and Chinese Academy of Medical Sciences, P.O.Box 2258, 100021, P.R., Beijing, China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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