一种高效且具有细胞活性的p53/hDM2相互作用的β-肽抑制剂。
A highly potent and cellularly active beta-peptidic inhibitor of the p53/hDM2 interaction.
作者信息
Hintersteiner Martin, Kimmerlin Thierry, Garavel Geraldine, Schindler Thorsten, Bauer Roman, Meisner Nicole-Claudia, Seifert Jan-Marcus, Uhl Volker, Auer Manfred
机构信息
The University of Edinburgh, Centre for Translational and Chemical Biology, UK.
出版信息
Chembiochem. 2009 Apr 17;10(6):994-8. doi: 10.1002/cbic.200800803.
New and improved: The incorporation of a 6-chlorotryptophan (6-Cl-Trp) into a beta-peptide (M)-3(14) helix 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.
新进展与改进
将6-氯色氨酸（6-Cl-Trp）掺入β-肽（M）-3(14)螺旋中可产生一种高亲和力的hDM2抑制剂，单分子分辨率的荧光涨落分析证明了这一点。当与穿膜肽缀合时，新得到的hDM2结合剂在体外可特异性抑制肿瘤细胞生长。
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