Journal of University of Science and Technology of China ›› 2016, Vol. 46 ›› Issue (10): 832-837.DOI: 10.3969/j.issn.0253-2778.2016.10.006

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Expression of an Azurin mutant and its interaction with a prodrug of cisplatin

LIU Xiaoxuan   

  1. 1.School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China; 2.Department of Chemistry, University of Science and Technology of China, Hefei 230026, China; 3.Institute of Life Sciences, Southeast University, Nanjing 210096, China
  • Received:2016-04-22 Revised:2016-06-07 Online:2016-10-31 Published:2016-10-31

Abstract: Azurin is a copper protein and possesses antitumor activity. The H117G mutant of Azurin (Az-H117G) was prepared, which is capable to bind exogenous imidazole or histidine. The interaction of Az-H117G with imidazole-based derivatives was investigated using UV-vis spectroscopy. Results show that the protein mutant can bind imidazole, histidine and Pt-His complex, a Pt(IV) prodrug of cisplatin. Based on this information, the protein/drug conjugate was prepared and the anti-proliferation of tumor cells was studied. The result indicates that this protein/drug conjugate might be potentially applicable to antitumor drug design.

Key words: cisplatin, prodrug, Azurin