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

Paper ID

PAPER000329

Year

2021

DOI

10.1016/j.ijpharm.2021.120940

PMID

34310959

Journal

International Journal of Pharmaceutics

Source URL

Experiments

• EXP001975 with Ab-CPP-LSP-siRNA (cetuximab–PEG–LMWP–AANL–siRNA; ARC) (siRNA (anti-EGFP; thiol-modified; Cy3/TAMRA labeled variants used for imaging))
• EXP001976 with CPP-LSP-siRNA (PEG–LMWP–AANL–siRNA; no antibody) (siRNA (anti-EGFP; thiol-modified; Cy3/TAMRA labeled variants used for imaging))
• EXP001977 with CPP-LSP/siRNA physical mixture (LMWP-AANL + siRNA complex) (siRNA (anti-EGFP; thiol-modified; Cy3/TAMRA labeled variants used for imaging))
• EXP001978 with Ab-CPP-MSP-siRNA (cetuximab–PEG–LMWP–GGPLGVR–siRNA; ARC) (siRNA (anti-EGFP; thiol-modified; Cy3/TAMRA labeled variants used for imaging))
• EXP001979 with Ab-CPP-siRNA (cetuximab–PEG–LMWP–siRNA; no substrate control) (siRNA (anti-EGFP; thiol-modified; Cy3/TAMRA labeled variants used for imaging))
• EXP001980 with Ab-CPP-LSP-siRNA-Cy3 (ARC; cetuximab–PEG–LMWP–AANL–siRNA) (siRNA (anti-EGFP; thiol-modified; Cy3/TAMRA labeled variants used for imaging))
• EXP001981 with CPP-LSP-siRNA-Cy3 (PEG–LMWP–AANL–siRNA; no antibody) (siRNA (anti-EGFP; thiol-modified; Cy3/TAMRA labeled variants used for imaging))
• EXP001982 with CPP-LSP-siRNA-Cy3/Ab physical mixture (noncovalent antibody addition) (siRNA (anti-EGFP; thiol-modified; Cy3/TAMRA labeled variants used for imaging))