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. Author manuscript; available in PMC: 2018 Aug 6.
Published in final edited form as: Mol Pharm. 2018 Feb 26;15(8):2892–2899. doi: 10.1021/acs.molpharmaceut.7b00765

Table 1.

Performance metrics of “clicked” gene therapeutics compared to other methods.

# Oligonucleotide/
small
molecule
Mechanism of
action/Target
Modification Stability
in
biofluids
Specificity Uptake
efficacy
Ref
1 MO-DM2 Antisense/r(CCUG) repeat expansion morpholino ++ +++ ++ 49
2 PMO-CPP antisense morpholino nd nd +++ 50
3 P-gp siRNA siRNA/reducing Pgp expression in breast cancer “Clicked” triblock copolymer, natural siRNA + ++ +++ 51
4 CD206-siRNA siRNA/macrophage targeted delivery Micelle mannosylation by click ++ +++ +++ 52
5 LW6 HIV-1 α supressing Click with a fluorophore nd nd +++ 53
6 D/Gal Induced gene expression/cancer cell Clicked galactose nd ++ ++ 54
7 ADC anti-CD22 antibody with doxorubicin/lymph oma cancer cell - ++ +++ +++ 55

+ Moderate, ++ High, +++ Very high