当前位置: X-MOL 学术Bioorg. Med. Chem. Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
d-Amino acid mutation of PMI as potent dual peptide inhibitors of p53-MDM2/MDMX interactions
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2017-09-07 , DOI: 10.1016/j.bmcl.2017.09.014
Xiang Li , Chao Liu , Si Chen , Honggang Hu , Jiacan Su , Yan Zou

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.



中文翻译:

d -PMI的氨基酸突变作为p53-MDM2 / MDMX相互作用的有效双肽抑制剂

根据先前报道的有效的双-肽P53-MDM2 / MDMX相互作用的PMI,一系列d -氨基酸突变PMI类似物,PMI-1 - 4,具有增强的蛋白水解抗性和体外肿瘤细胞抑制活性进行了报道,其中脂质体-PMI-1对U87细胞系的抑制活性强于Nutlin-3。这种d-氨基酸突变策略可以帮助提高肽药物的潜力。

更新日期:2017-09-07
down
wechat
bug