d-Amino acid mutation of PMI as potent dual peptide inhibitors of p53-MDM2/MDMX interactions |
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| Authors: | Xiang Li Chao Liu Si Chen Honggang Hu Jiacan Su Yan Zou |
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| Affiliation: | 1. Department of Organic Chemistry, College of Pharmacy, Second Military Medical University, Shanghai 200433, People’s Republic of China;2. Institute of Human Virology, University of Maryland School of Medicine, 725 West Lombard Street, Baltimore, MD 21201, United States;3. Changhai Hospital, Second Military Medical University, Shanghai 200433, People’s Republic of China |
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| Abstract: | ![]()
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. |
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| Keywords: | PMI P53 MDM2/MDMX Peptides Tumor |
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