Turning a scorpion toxin into an antitumor miniprotein.
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ABSTRACT:
SUBMITTER: Li C
PROVIDER: S-EPMC3810402 | biostudies-literature | 2008 Oct
REPOSITORIES: biostudies-literature
Publications
Turning a scorpion toxin into an antitumor miniprotein.
Li Chong C Liu Min M Monbo Juahdi J Zou Guozhang G Li Changqing C Yuan Weirong W Zella Davide D Lu Wei-Yue WY Lu Wuyuan W
Journal of the American Chemical Society 20080918 41
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-re ...[more]
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