Abstract: Receptor can specifically bind its ligand with high affinyty.Based on this antisense oligonucleotides(ONs) linked to specific receptor ligand can be targeted to cells which possess specific receptor and enter into these cells by receptor-mediated endocytosis.Adequate intracellular concentrations of antisense ONs can be obtained enough to inhibit target gene expression. Receptors used frequently, formation of ONs delivery complexes, questions required to settle in the process of endocytosis and experiment studies of receptor mediated antisense therapy are concisely introduced in this article.