Institute of Human Virology, University of Maryland School of Medicine, 725 W. Lombard St., Baltimore, MD 21201, USA.
Angew Chem Int Ed Engl. 2009;48(46):8712-5. doi: 10.1002/anie.200904550.
[Image: see text] 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.
[图像：见正文]癌蛋白 MDM2 和 MDMX 负调控肿瘤抑制蛋白 p53 的活性和稳定性，是抗癌治疗的重要分子靶点。将对 MDM2/MDMX 结合至关重要的四个残基嫁接至蜂毒神经毒素的 C 端α-螺旋，将其转化为具有潜在抗肿瘤活性的新型强效 p53 激活剂。
