2'-O-[2-(amino)-2-oxoethyl] oligonucleotides |
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| Authors: | Prakash Thazha P Kawasaki Andrew M Lesnik Elena A Owens Stephen R Manoharan Muthiah |
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| Institution: | Department of Medicinal Chemistry, Isis Pharmaceuticals Inc., 2292 Faraday Avenue, Carlsbad, California 92008, USA. |
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| Abstract: | structure: see text] Oligonucleotides with novel modifications, 2'-O-2-(amino)-2-oxoethyl] (2'-O-NAc), 2'-O-2-(methylamino)-2-oxoethyl] (2'-O-NMAc), 2'-O-2-(dimethylamino)-2-oxoethyl] (2'-O-DMAc), and 2'-O-2-2-(dimethylamino)ethyl]amino]-2-oxoethyl] (2'-O-DMAEAc), have been synthesized. These modified oligonucleotides exhibit high binding affinity to complementary RNA (and not to DNA) and considerably enhance the nuclease stability of oligonucleotides with t(1/2) > 24 h. |
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