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

Journal article

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.

Authors: Geng, L; Wang, Z; Jia, X; Han, Q; Xiang, Z

• Publication status: Published
• Peer review status: Peer reviewed
• Publisher: Ivyspring International Publisher
• Journal: Theranostics
• Volume: 6
• Issue: 8
• Pages: 1261-1273
• Publication date: 2016-05-28
• DOI: 10.7150/thno.14302
• EISSN: 1838-7640
• ISSN: 1838-7640
• Language: English
• Keywords: In vivo; Biology; Molecular biology; Chemistry; Doxorubicin; Breast cancer; Human Epidermal Growth Factor Receptor 2; Drug delivery; Biochemistry; Cancer research; Peptide; In vitro; Peptide library; Phage display; Medicine; Peptide sequence; Cancer; Targeted drug delivery; Ex vivo