Design, Synthesis, and Activity Evaluation of a New 5-fluorouracil Prodrug Containing an Asn-Gly-Arg(NO2)COOCH3 Tripeptide

Title:Design, Synthesis, and Activity Evaluation of a New 5-fluorouracil Prodrug Containing an Asn-Gly-Arg(NO2)COOCH3 Tripeptide

Volume: 19 Issue: 10

Author(s): Yepeng Luan, Fanbo Jing, Jian Zhang, Mingming Zou, Xuejian Wang, Yuping Jia, Ning Liu, Jiajia Mou and Wenfang Xu

Affiliation:

Keywords: Aminopeptidase N, NGR, 5-fluorouracil, antitumor, angiogenesis, metastasis, tumor cells, tumor-homing tripeptide, 5-fluorouracil

Abstract: Aminopeptidase N (APN/CD13) of the M1 family is a broad specificity enzyme that is intimately involved in tumor angiogenesis and metastasis. Asparagine–glycine–arginine (NGR) is a tumor-homing tripeptide, which can selectively combine with APN/CD13 that is overexpressed on the surface of some tumor cells. Various anti-tumor drugs can be conjugated to NGR to improve selectivity, efficacy, and to decrease drug toxicity. In this study, a tripeptide NGR(NO2) was synthesized and conjugated with 5-fluorouracil. The anti-tumor activities of this new prodrug were evaluated in vivo. More significant anti-tumor effects were observed over the parent 5-fluorouracil.

Cite this article as:

Luan Yepeng, Jing Fanbo, Zhang Jian, Zou Mingming, Wang Xuejian, Jia Yuping, Liu Ning, Mou Jiajia and Xu Wenfang, Design, Synthesis, and Activity Evaluation of a New 5-fluorouracil Prodrug Containing an Asn-Gly-Arg(NO2)COOCH3 Tripeptide, Protein & Peptide Letters 2012; 19 (10) . https://dx.doi.org/10.2174/092986612802762615