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EXP001975

Paper

Antibody-siRNA conjugates (ARCs) using multifunctional peptide as a tumor enzyme cleavable linker mediated effective intracellular delivery of siRNA (2021)

Peptide

Ab-CPP-LSP-siRNA (cetuximab–PEG–LMWP–AANL–siRNA; ARC)

Sequence: VSRRRRGGRRRRRRAANL

RNA

siRNA (anti-EGFP; thiol-modified; Cy3/TAMRA labeled variants used for imaging)

All experiment fields

Experiment Id EXP001975
Paper Antibody-siRNA conjugates (ARCs) using multifunctional peptide as a tumor enzyme cleavable linker me
Peptide Ab-CPP-LSP-siRNA (cetuximab–PEG–LMWP–AANL–siRNA; ARC)
Delivery Success Class no
In Vivo Flag no
Uptake Confirmed yes
Label Confidence high
In Vitro Functional Effect yes
Endosomal Escape Evidence
Peptide Concentration Defined by conjugate; compared at equal siRNA dose (100 nM).
Rna Concentration 100 nM siRNA for all transfection groups (24 h treatment + 72 h incubation before readout).
Mixing Ratio Covalent conjugate (ARC).
Formulation Format Antibody–multifunctional peptide–siRNA covalent conjugate (ARC)
Formulation Components Cetuximab linked to PEG–LMWP–AANL–anti-EGFP siRNA.
Size Nm
Zeta Mv
Model Scope in_vitro
Model Type in vitro
Cell Lines Or Primary Cells HCT116-EGFP (EGFP stable transfectant human colon cancer cells)
Animal Model
Administration Route
Output Type In vitro functional RNA effect (EGFP silencing) by confocal + western blot
Output Value ~85.7% EGFP protein silencing (western blot); strongest silencing among tested groups.
Output Units
Output Notes Activation via tumor enzyme legumain cleavage of AANL; antibody masks CPP during circulation in design concept.
Toxicity Notes MTT assay in HCT116: ~90% viability at 125 nM; >75% up to 500 nM (siRNA-equivalent).
Curation Notes