Abstract: Oligonucleotides such as antisense oligonucleotides (ASOs), small interfering RNA (siRNA) and aptamer can achieve the purpose of treating diseases by targeting pathogenic RNA or protein and inhibiting its activity, but many types of oligonucleotides have such disadvantages as poor active targeting, instability in vivo and poor transmembrane ability, so on the basis of traditional oligonucleotides, the functions and properties of nucleic acid molecules are improved by covalently coupling oligonucleotides with other functional molecules, e.g., improving cell uptake, tissue delivery, bioavailability, catalytic effect, etc., and thereby improving the effect of therapeutic nucleic acid. This article focuses on the development of oligonucleotide conjugates in two directions of delivery and catalytic degradation, and reviews the latest research progress of 7 typical oligonucleotide conjugates, so as to provide some insights and reference for structural design and further clinical application of oligonucleotide conjugates.