Design of RGD-ATWLPPR peptide conjugates for the dual targeting of αV β3 integrin and neuropilin-1

Organic & Biomolecular Chemistry
Fabien ThoreauDidier Boturyn

Abstract

Targeting the tumour microenvironment is a promising strategy to detect and/or treat cancer. The design of selective compounds that co-target several receptors frequently overexpressed in solid tumours may allow a reliable and selective detection of tumours. Here we report the modular synthesis of compounds encompassing ligands of αVβ3 integrin and neuropilin-1 that are overexpressed in the tumour microenvironment. These compounds were then evaluated through cellular experiments and imaging of tumours in mice. We observed that the peptide that displays both ligands is more specifically accumulating in the tumours than in controls. Simultaneous interaction with αVβ3 integrin and NRP1 induces NRP1 stabilization at the cell membrane surface which is not observed with the co-injection of the controls.

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Citations

Dec 7, 2018·ChemMedChem·Fatima HamdanSaeed Balalaie
Feb 6, 2019·International Journal of Molecular Sciences·Stephan Niland, Johannes A Eble

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Methods Mentioned

BETA
ELISA
Assay
confocal microscopy
Protein Assay

Software Mentioned

Image J®

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