使用反向p53肽作为MDM2的抑制剂。
Use of a retroinverso p53 peptide as an inhibitor of MDM2.
作者信息
Sakurai Kaori, Chung Hak Suk, Kahne Daniel
机构信息
Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA.
出版信息
J Am Chem Soc. 2004 Dec 22;126(50):16288-9. doi: 10.1021/ja044883w.
PMID:15600307
Abstract
An N-terminal helical region of the tumor suppressor p53 binds in a hydrophobic cleft of the oncoprotein MDM2. A retroinverso isomer of the natural N-terminal helical peptide was found to interact with MDM2 using the same hydrophobic residues, Phe, Trp, and Leu. We propose that the retroinverso d-peptide adopts a right-handed helical conformation to achieve functional mimicry of the p53 peptide.
摘要
肿瘤抑制蛋白p53的N端螺旋区域结合在癌蛋白MDM2的疏水裂隙中。发现天然N端螺旋肽的反向异构体利用相同的疏水残基苯丙氨酸、色氨酸和亮氨酸与MDM2相互作用。我们提出，反向d-肽采用右手螺旋构象以实现p53肽的功能模拟。
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