Apamin as a template for structure-based rational design of potent peptide activators of p53.
Apamin as a template for structure-based rational design of potent peptide activators of p53.
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DOI:
10.1002/anie.200904550
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发表时间:
2009
影响因子:
16.6
通讯作者:
Lu, Wuyuan
中科院分区:
文献类型:
--
作者:
Li, Chong;Pazgier, Marzena;Liu, Min;Lu, Wei-Yue;Lu, Wuyuan
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 critical for MDM2/MDMX binding to the C-terminal α-helix of apamin converts the bee-venom neurotoxin into a novel class of potent p53 activators with potential antitumor activity.
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