| Turning a scorpion toxin into an antitumor miniprotein. | |
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MedLine Citation:
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PMID: 18798622 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The oncoproteins MDM2 and MDMX negatively regulate the activity and stability of the tumor suppressor protein p53 and are important molecular targets for anticancer therapy. Grafting four residues of p53 critical for MDM2/MDMX binding to the N-terminal alpha-helix of BmBKTx1, a scorpion toxin isolated from the venom of the Asian scorpion Buthus martensi Karsch, converts the miniature protein into an effective inhibitor of p53 interactions with MDM2 and MDMX. Additional mutations enable the 27-residue miniprotein inhibitor to traverse the cell membrane and selectively kill tumor cells in a p53 dependent manner. |
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Authors:
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Chong Li; Min Liu; Juahdi Monbo; Guozhang Zou; Changqing Li; Weirong Yuan; Davide Zella; Wei-Yue Lu; Wuyuan Lu |
Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2008-09-18 |
Journal Detail:
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Title: Journal of the American Chemical Society Volume: 130 ISSN: 1520-5126 ISO Abbreviation: J. Am. Chem. Soc. Publication Date: 2008 Oct |
Date Detail:
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Created Date: 2008-10-08 Completed Date: 2008-12-17 Revised Date: 2009-01-22 |
Medline Journal Info:
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Nlm Unique ID: 7503056 Medline TA: J Am Chem Soc Country: United States |
Other Details:
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Languages: eng Pagination: 13546-8 Citation Subset: IM |
Affiliation:
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Institute of Human Virology, University of Maryland School of Medicine, 725 West Lombard Street, Baltimore, Maryland 21201, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Amino Acid Sequence Animals Antineoplastic Agents / chemistry* Models, Molecular Protein Structure, Tertiary Scorpion Venoms / chemistry* Scorpions / chemistry* Structural Homology, Protein |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 0/Scorpion Venoms |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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