Prakash Thazha P, Kraynack Bryan, Baker Brenda F, Swayze Eric E, Bhat Balkrishen
Department of Medicinal Chemistry, Isis Pharmaceuticals, Inc., Carlsbad, CA 92008, USA.
Bioorg Med Chem Lett. 2006 Jun 15;16(12):3238-40. doi: 10.1016/j.bmcl.2006.03.053. Epub 2006 Apr 17.
Synthetic small interfering RNA (siRNA) mediated silencing of a specific gene is emerging as a powerful tool for gene regulation. However, their utility is limited for therapeutic applications primarily due to poor stability. The 2',5'-linked oligonucleotides are known to be more stable to nucleolytic degradation than 3',5'-linked oligonucleotides. The 2',5'-linkage is tolerated in the sense strand of the siRNA duplex. However, the 2',5'-linkage is not tolerated in the antisense strand of the siRNA duplex.
合成小干扰RNA(siRNA)介导的特定基因沉默正成为一种强大的基因调控工具。然而,由于稳定性差,它们在治疗应用中的效用受到限制。已知2',5'-连接的寡核苷酸比3',5'-连接的寡核苷酸对核酸酶降解更稳定。2',5'-连接在siRNA双链体的有义链中是可耐受的。然而,2',5'-连接在siRNA双链体的反义链中是不可耐受的。