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<p>Conjugation techniques are central to improving
intracellular delivery of bioactive small molecules. However, tracking
and assessing the overall biological outcome of these constructs
remains poorly understood. We addressed this issue by having
developed a focused library of heterobivalent constructs based on
Rho kinase inhibitors to probe various scenarios. By comparing
induction of a phenotype of interest vs. cell viability vs. cellular uptake,
we demonstrate that such conjugates indeed lead to divergent cellular
outcomes.
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Intracellular Delivery of Peptidyl Ligands by Reversible Cyclization: Discovery of a PDZ Domain Inhibitor that Rescues CFTR Activity
