An octopus-mimic PEGylated peptide as a specific integrin αvβ3 inhibitor for preventing tumor progression

Xue Shan; Lei Zhang; Yurui Xu; Lei Sun; Leilei Guo; Shujun Feng; Haixiong Ge; Tingting Gu; Xinghai Ning

doi:10.1039/c9cc09496b

An octopus-mimic PEGylated peptide as a specific integrin αvβ3 inhibitor for preventing tumor progression

Chem Commun (Camb). 2020 Feb 18;56(14):2178-2181. doi: 10.1039/c9cc09496b. Epub 2020 Jan 23.

Authors

Xue Shan¹, Lei Zhang², Yurui Xu¹, Lei Sun¹, Leilei Guo³, Shujun Feng¹, Haixiong Ge⁴, Tingting Gu¹, Xinghai Ning¹

Affiliations

¹ National Laboratory of Solid State Microstructures, College of Engineering and Applied Sciences, Nanjing University, Nanjing 210093, China. haixiong@nju.edu.cn gutingting@nju.edu.cn xning@nju.edu.cn and Chemistry and Biomedicine Innovation Center (ChemBIC), Nanjing University, Nanjing 210093, China.
² National Laboratory of Solid State Microstructures, College of Engineering and Applied Sciences, Nanjing University, Nanjing 210093, China. haixiong@nju.edu.cn gutingting@nju.edu.cn xning@nju.edu.cn and Chemistry and Biomedicine Innovation Center (ChemBIC), Nanjing University, Nanjing 210093, China and The Center of Diagnosis and Treatment for Joint Disease, Drum Tower Hospital Affiliated to Medical School of Nanjing University, Nanjing 210093, China.
³ State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, Center of Drug Discovery, Center of Advanced Pharmaceutics and Biomaterials, China Pharmaceutical University, Nanjing 210009, China.
⁴ National Laboratory of Solid State Microstructures, College of Engineering and Applied Sciences, Nanjing University, Nanjing 210093, China. haixiong@nju.edu.cn gutingting@nju.edu.cn xning@nju.edu.cn.

PMID: 31971174
DOI: 10.1039/c9cc09496b

Abstract

We have developed a multivalent PEGylated RWrNR, named octopus-R, which exhibits good water solubility, biostability, biocompatibility and cancer targeting ability, endowing it with high anticancer potential. Octopus-R represents a promising theranostic agent and holds great potential for improving the management of malignant tumors.

MeSH terms

Animals
Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Integrin alphaVbeta3 / antagonists & inhibitors*
Integrin alphaVbeta3 / metabolism
Mice
Mice, Nude
Neoplasms, Experimental / drug therapy
Neoplasms, Experimental / metabolism
Neoplasms, Experimental / pathology
Peptides / chemical synthesis
Peptides / chemistry
Peptides / pharmacology*
Polyethylene Glycols / chemical synthesis
Polyethylene Glycols / chemistry
Polyethylene Glycols / pharmacology*
Structure-Activity Relationship

Substances

Antineoplastic Agents
Integrin alphaVbeta3
Peptides
Polyethylene Glycols