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

Theranostics
Yi MaYueqing Gu

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 vivopeptide-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.

Citations

Dec 13, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Hernando CurtidorManuel E Patarroyo
Dec 14, 2019·Nuclear Medicine Communications·Mohammadali RamezanizadehFariba Maleki
Mar 3, 2020·Nanoscale Horizons : the Home for Rapid Reports of Exceptional Significance in Nanoscience and Nanotechnolgy·Emilie DarriguesAnaliz Rodriguez
Apr 13, 2021·Journal of Biomechanics·Mohan YasodharababuArun K Nair
May 18, 2021·Frontiers in Bioengineering and Biotechnology·Zeynep KaragözAurélie Carlier

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Methods Mentioned

BETA
flow cytometry
fluorescence imaging
confocal
FCS
xenograft

Software Mentioned

GraphPad
Discovery Studio ( DS )
LibDock
chemBioDraw
RWrNM
Prism
Pro32
CDOCKER
GraphPad Prism
Discovery

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