A Highly Potent and Cellularly Active β-Peptidic Inhibitor of the p53/hDM2 Interaction
A Highly Potent and Cellularly Active β-Peptidic Inhibitor of the p53/hDM2 Interaction
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DOI：
10.1002/cbic.200800803
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发表时间：
2009-04-14
期刊：
影响因子：
3.2
通讯作者：
Auer, Manfred
中科院分区：
文献类型：
--
作者：
Hintersteiner, Martin;Kimmerlin, Thierry;Auer, Manfred
新的和改进的：6-氯色氨酸（6-Cl-Trp）与β-肽（M）-314螺旋的结合产生了高亲和力的hDM 2抑制剂，如单分子分辨率的荧光波动分析所示。当与穿透素缀合时，新衍生的hDM 2结合剂在体外特异性抑制肿瘤细胞生长。
New and improved: The incorporation of a 6‐chlorotryptophan (6‐Cl‐Trp) into a β‐peptide (M)‐314helix leads to a high‐affinity hDM2 inhibitor, as demonstrated by fluorescence fluctuation analysis at single molecule resolution. When conjugated to penetratin, the newly derived hDM2 binder specifically inhibits tumour cell growth in vitro.