Synthesis and biological properties of DNA-sugar conjugates.
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 resistance against nuclease digestion and the membrane permeability of the conjugates.
Yokoyama
K
K
Department of Environmental and Biological Chemistry, Kyushu School of Engineering, Kinki University.
Kubo
T
T
Dubey
K K
KK
Takeshita
K
K
Kanno
K
K
Fujii
M
M
D000606:Amino Sugars / Q000737:chemistry*; D002463:Cell Membrane Permeability; D004247:DNA / Q000737:chemistry; D004720:Endonucleases / Q000378:metabolism; D009693:Nucleic Acid Hybridization; D020319:Oligodeoxyribonucleotides, Antisense / Q000138:chemical synthesis* / Q000737:chemistry* / Q000378:metabolism
D000606:Amino Sugars; D020319:Oligodeoxyribonucleotides, Antisense; D004247:DNA; D004720:Endonucleases