© 2001 by Oxford University Press
Synthesis and biological properties of DNA-sugar conjugates
1 Department of Environmental and Biological Chemistry, Kyushu School of Engineering, Kinki University, 2 Henkel Research Center of Advanced Technology, Molecular Engineering Institute, Kinki University
In order to improve the pharmacological properties of antisense and antigene oligonucleotides, oligodeoxynucleotides conjugated with amino sugars at the 5'-terminus were synthesized by solid phase fragment condensation (SPFC) method. The obtained DNA-sugar conjugates were evaluated in their chemical and biological activities to show that 5'-end modification of oligonucleotides with sugars enhanced the thermal stability of the hybrid duplex with complementary DNA, the registance against nuclease digestion and the membrane permeability of the conjugates.