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Design and synthesis of AApeptides: a new class of peptide mimics |
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| Authors: | Hu Yaogang Li Xiaolong Sebti Said M Chen Jiandong Cai Jianfeng |
| Affiliation: | a Department of Chemistry, University of South Florida, 4202 E. Fowler Ave, CHE 205, Tampa, FL 33620, USA b Molecular Oncology Department, Moffitt Cancer Center, 12902 Magnolia Drive, Tampa, FL 33612, USA c Drug Discovery Department, Moffitt Cancer Center, 12902 Magnolia Drive, Tampa, FL 33612, USA |
| Abstract: | A new family of peptide mimics termed ‘AApeptides’, which are oligomers of N-acylated-N-aminoethyl amino acids, was proposed. The design and efficient synthesis of AApeptides are described. As proof-of-the-concept, we show that AApeptides can inhibit p53/MDM2 protein-protein interaction with significant activity (IC50 = 38 μM) and specificity. Preliminary data also demonstrates that AApeptides are resistant to enzymatic hydrolysis. With the ease of synthesis and diversification, potent bioactivity, and resistance to proteolysis, the development of sequence-specific AApeptides may expand the potential biomedical applications of peptidomimetics. |
| Keywords: | Peptidomimetics AApeptides Protein-protein interactions p53/MDM2 interaction ELISA |
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