Theranostics 2017; 7(6):1511-1523. doi:10.7150/thno.18401 This issue Cite

Research Paper

Novel Linear Peptides with High Affinity to αvβ3 Integrin for Precise Tumor Identification

Yi Ma*, Guanhua Ai*, Congying Zhang*, Menglu Zhao, Xue Dong, Zhihao Han, Zhaohui Wang, Min Zhang, Yuxi Liu, Weidong Gao, Siwen Li, Yueqing Gu

State Key Laboratory of Natural Medicines, Department of Biomedical Engineering, School of Engineering, China Pharmaceutical University, Nanjing, 24 Tongjia Road, 210009 (China).
* These authors contributed equally to this work

Citation:
Ma Y, Ai G, Zhang C, Zhao M, Dong X, Han Z, Wang Z, Zhang M, Liu Y, Gao W, Li S, Gu Y. Novel Linear Peptides with High Affinity to αvβ3 Integrin for Precise Tumor Identification. Theranostics 2017; 7(6):1511-1523. doi:10.7150/thno.18401. https://www.thno.org/v07p1511.htm
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Abstract

Graphic abstract

Development of alternative linear peptides for targeting αvβ3 integrin has attracted much attention, as the traditional peptide ligand, cyclic RGD, is limited by inferior water-solubility and complex synthesis. Using pharmacophore-based virtual screening and high-throughput molecular docking, we identified two novel linear small peptides RWr and RWrNM with high affinity and specificity to αvβ3 integrin. The competitive binding with cyclic RGD (c(RGDyK)) and cellular uptake related to the integrin expression levels verified their affinity to αvβ3 integrin. The intermolecular interaction measurement and dynamics simulation demonstrated the high binding affinity and stability, especially for RWrNM. In vivo peptide-guided tumor imaging and targeted therapy further confirmed their specificity. Results indicated that the newly identified small linear peptide RWrNM, with high affinity and specificity to αvβ3 integrin, better water-solubility, and simplified synthetic process, could overcome limitations of the current cyclic RGD peptides, paving the way for diverse use in diagnosis and therapy.

Keywords: αvβ3 integrin, linear peptide, binding affinity.


Citation styles

APA
Ma, Y., Ai, G., Zhang, C., Zhao, M., Dong, X., Han, Z., Wang, Z., Zhang, M., Liu, Y., Gao, W., Li, S., Gu, Y. (2017). Novel Linear Peptides with High Affinity to αvβ3 Integrin for Precise Tumor Identification. Theranostics, 7(6), 1511-1523. https://doi.org/10.7150/thno.18401.

ACS
Ma, Y.; Ai, G.; Zhang, C.; Zhao, M.; Dong, X.; Han, Z.; Wang, Z.; Zhang, M.; Liu, Y.; Gao, W.; Li, S.; Gu, Y. Novel Linear Peptides with High Affinity to αvβ3 Integrin for Precise Tumor Identification. Theranostics 2017, 7 (6), 1511-1523. DOI: 10.7150/thno.18401.

NLM
Ma Y, Ai G, Zhang C, Zhao M, Dong X, Han Z, Wang Z, Zhang M, Liu Y, Gao W, Li S, Gu Y. Novel Linear Peptides with High Affinity to αvβ3 Integrin for Precise Tumor Identification. Theranostics 2017; 7(6):1511-1523. doi:10.7150/thno.18401. https://www.thno.org/v07p1511.htm

CSE
Ma Y, Ai G, Zhang C, Zhao M, Dong X, Han Z, Wang Z, Zhang M, Liu Y, Gao W, Li S, Gu Y. 2017. Novel Linear Peptides with High Affinity to αvβ3 Integrin for Precise Tumor Identification. Theranostics. 7(6):1511-1523.

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