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. Author manuscript; available in PMC: 2020 Nov 20.
Published in final edited form as: Bioconjug Chem. 2019 Oct 22;30(11):2947–2957. doi: 10.1021/acs.bioconjchem.9b00640

Figure 5.

Figure 5.

a.) The ProGlo delivered by ND-ProGlo is able to enter the cytoplasm and interact with its target receptor (PR). ND-ProGlo is able to stimulate significantly higher levels of PR signaling than ProGlo in luciferase gene reporter assays, indicating greater cytoplasmic delivery and receptor activation. This activity was abolished by pre-incubation with tight binding PR-inhibitor RU486. ND-ProGlo requires much higher concentration to achieve similar signal to positive control P4 (progesterone), consistent with previous results. b) The role of PR in ND-mediated delivery of ProGlo was evaluated using receptor blocking experiments. Consistent with expectations, cytoplasmic PR plays little role in the delivery of ProGlo to the cytoplasm. The proposed method of selective accumulation is increased retention due to interactions between ProGlo and PR after delivery.