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. 2017 Oct 23;45(21):12388–12400. doi: 10.1093/nar/gkx960

Figure 1.

Figure 1.

Uptake and activity of parent and GalNAc-conjugated ASOs. (A) Uptake of parent and GalNAc-conjugated phosphorothioate ASOs in three hepatocyte cell culture models. Increased uptake of the GalNAc ASO conjugate and competition by free GalNAc is observed in ASGR-expressing cells, HepG2 and primary murine hepatocytes, but not the ASGR null cell line Huh-7. (B) Uptake of parent and GalNAc-conjugated phosphodiester ASOs in three hepatocyte cell culture models. Uptake of the GalNAc ASO conjugate and competition by free GalNAc is observed in ASGR-expressing cells, HepG2 and primary murine hepatocytes, but not the ASGR null cell line Huh-7. (C) Knockdown activity parent and GalNAc-conjugated phosphorothioate ASOs in three hepatocyte cell culture models. Increased potency of the GalNAc–ASO conjugate is observed only in primary murine hepatocytes.