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Cellular uptake of antisense oligonucleotides.

Antisense oligonucleotides (AS ONs) selectively bind to the target mRNA and prevent its translation into the corresponding protein. Various tissue culture studies demonstrated that AS ONs enter into cells via the receptor-mediated endocytosis pathway. There are many different types of receptors, and their characteristics and expression vary with cell types. In this review, we will discuss the characteristics of the various receptors that have been isolated in vitro. We will also discuss the uptake and the bioavailability of AS ONs after being administered in vivo.