Drug “Clicking” on Cell-Penetrating Fluorescent Nanoparticles for In Cellulo Chemical Proteomics,Bioconjugate Chemistry

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Drug “Clicking” on Cell-Penetrating Fluorescent Nanoparticles for In Cellulo Chemical Proteomics
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2018-08-18 00:00:00 , DOI: 10.1021/acs.bioconjchem.8b00481
Teresa Valero _{1,

2,

3} , Antonio Delgado-González _{2,

3} , Juan Diego Unciti-Broceta _{2,

4} , Victoria Cano-Cortés _{2,

3} , Ana M. Pérez-López ₁ , Asier Unciti-Broceta ₁ , Rosario M. Sánchez Martín _{2,

3}

Affiliation

Chemical proteomics approaches are widely used to identify molecular targets of existing or novel drugs. This manuscript describes the development of a straightforward approach to conjugate azide-labeled drugs via click chemistry to alkyne-tagged cell-penetrating fluorescent nanoparticles as a novel tool to study target engagement and/or identification inside living cells. A modification of the Baeyer test for alkynes allows monitoring the Cu(I)-catalyzed azide–alkyne cycloaddition (CuAAC) reaction, guaranteeing the presence of the drug on the solid support. As a proof of concept, the conjugation of the promiscuous kinase inhibitor dasatinib to Cy5-labeled nanoparticles is presented. Dasatinib-decorated fluorescent nanoparticles efficiently inhibited its protein target SRC in vitro, entered cancer cells, and colocalized with SRC in cellulo.

更新日期：2018-08-18

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