D-Amino acid mutation of PMI as potent dual peptide inhibitors of p53-MDM2/MDMX interactions

被引：11

作者：

Li, Xiang ^{[1
,2
]}

Liu, Chao ^{[1
]}

Chen, Si ^{[1
]}

Hu, Honggang ^{[1
]}

Su, Jiacan ^{[3
]}

Zou, Yan ^{[1
]}

机构：

[1] Second Mil Med Univ, Dept Organ Chem, Coll Pharm, Shanghai 200433, Peoples R China

[2] Univ Maryland, Inst Human Virol, Sch Med, 725 West Lombard St, Baltimore, MD 21201 USA

[3] Second Mil Med Univ, Changhai Hosp, Shanghai 200433, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 20期

关键词：

PMI; P53; MDM2/MDMX; D-Amino acid; Peptides; Tumor; P53; MDM2; CANCER; THERAPY;

D O I：

10.1016/j.bmcl.2017.09.014

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

According to the previously reported potent dual L-peptide PMI of p53-MDM2/MDMX interactions, a series of D-amino acid mutational PMI analogues, PMI-1-4, with enhanced proteolytic resistence and in vitro tumor cell inhibitory activities were reported, of which Liposome-PMI-1 showed a stronger inhibitory activity against the U87 cell lines than Nutlin-3. This D-amino acid mutation strategy may give a hand for enhancing the potential of peptide drugs. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：4678 / 4681

页数：4

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