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Labeling of VEGFR1D2 through oxime ligation.

Abstract：

:We reported an useful protocol for the labeling of the second domain of the Vascular Endothelial Growth Factor Receptor 1 (VEGFR1D2), a small protein ligand able to bind VEGF, the main regulator of angiogenesis. We developed a bioconjugation strategy based on the use of oxime-ligation reaction conjugating an aldehyde derivative of the VEGFR1D2 to a molecular probe harboring an alkoxyamine functional group. We applied the synthetic protocol to prepare a biotinylated conjugate of VEGFR1D2 and we demonstrate that the bioconjugate retains its ability to specifically bind its natural ligand, VEGF, with high affinity. The biotinylated VEGFR1D2 could be useful to detect and quantify VEGF for diagnostic purposes as well as a tool for the screening of new molecules targeting VEGFRs for therapeutic applications. The labeling protocol is versatile and can be extended to different molecular probes, such as fluorophores, chelators or multimeric scaffolds, affording a biomedical platform for VEGF targeting.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

De Rosa L,Di Stasi R,Longhitano L,D'Andrea LD

doi

10.1016/j.bioorg.2019.103160

subject

Has Abstract

pub_date

2019-10-01 00:00:00

pages

103160

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)30981-2

journal_volume

91

pub_type

杂志文章

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