Theranostics 2016; 6(8):1261-1273. doi:10.7150/thno.14302

Research Paper

HER2 Targeting Peptides Screening and Applications in Tumor Imaging and Drug Delivery

Lingling Geng1,3*, Zihua Wang1,2*, Xiangqian Jia1,4, Qiuju Han1,4, Zhichu Xiang1,2, Dan Li1,2, Xiaoliang Yang1,2, Di Zhang1, Xiangli Bu1,2, Weizhi Wang1,2✉, Zhiyuan Hu1,2✉, Qiaojun Fang1,2✉

1. CAS Key Laboratory for Biomedical Effects of Nanomaterials & Nanosafety, National Center for Nanoscience and Technology, Beijing 100190, China;
2. CAS Center for Excellence in Nanoscience, National Center for Nanoscience and Technology, Beijing 100190, China;
3. National Laboratory of Biomacromolecules, Institute of Biophysics, Chinese Academy of Sciences, Beijing 100101, China;
4. Pharmacy College, Liaoning Medical University, Jinzhou, Liaoning 121001, China.
*These authors contributed equally to this work.

Abstract

Herein, computational-aided one-bead-one-compound (OBOC) peptide library design combined with in situ single-bead sequencing microarray methods were successfully applied in screening peptides targeting at human epidermal growth factor receptor-2 (HER2), a biomarker of human breast cancer. As a result, 72 novel peptides clustered into three sequence motifs which are PYL***NP, YYL***NP and PPL***NP were acquired. Particularly one of the peptides, P51, has nanomolar affinity and high specificity for HER2 in ex vivo and in vivo tests. Moreover, doxorubicin (DOX)-loaded liposome nanoparticles were modified with peptide P51 or P25 and demonstrated to improve the targeted delivery against HER2 positive cells. Our study provides an efficient peptide screening method with a combination of techniques and the novel screened peptides with a clear binding site on HER2 can be used as probes for tumor imaging and targeted drug delivery.

Keywords: HER2 targeting peptide, tumor imaging, drug delivery, breast cancer, MD simulation.

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How to cite this article:
Geng L, Wang Z, Jia X, Han Q, Xiang Z, Li D, Yang X, Zhang D, Bu X, Wang W, Hu Z, Fang Q. HER2 Targeting Peptides Screening and Applications in Tumor Imaging and Drug Delivery. Theranostics 2016; 6(8):1261-1273. doi:10.7150/thno.14302. Available from http://www.thno.org/v06p1261.htm