Enzymatic hydrolysis and biological activity of oligonucleotides containing 5-substituted pyrimidine bases
Two series of alternating ODNs containing 5-n.alkyl-, alkenyl- and alkynyl-dU and -dC units have been prepared in order to study the kinetics of their hydrolysis by SV PDE and human serum, respectively. Both in (r5dUpdA)10 and (r5dCpdG)6 series the rate of hydrolysis decreased with increasing length...
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| Published in | Nucleosides & nucleotides Vol. 18; no. 6-7; pp. 1665 - 1666 |
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| Main Authors | , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
United States
01.06.1999
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| Subjects | |
| Online Access | Get full text |
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| Abstract | Two series of alternating ODNs containing 5-n.alkyl-, alkenyl- and alkynyl-dU and -dC units have been prepared in order to study the kinetics of their hydrolysis by SV PDE and human serum, respectively. Both in (r5dUpdA)10 and (r5dCpdG)6 series the rate of hydrolysis decreased with increasing length of side-chain. Replacement of thymidines by 5-hexynyl-dU in different antisense oligomers resulted in considerably higher biological activity relative to that of the thymidine-containing counterparts. |
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| AbstractList | Two series of alternating ODNs containing 5-n.alkyl-, alkenyl- and alkynyl-dU and -dC units have been prepared in order to study the kinetics of their hydrolysis by SV PDE and human serum, respectively. Both in (r5dUpdA)10 and (r5dCpdG)6 series the rate of hydrolysis decreased with increasing length of side-chain. Replacement of thymidines by 5-hexynyl-dU in different antisense oligomers resulted in considerably higher biological activity relative to that of the thymidine-containing counterparts. |
| Author | Sági, G Otvös, L Tóth, F D Sági, J Jeney, A Szemzõ, A |
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| SubjectTerms | Blood Humans Hydrolysis Kinetics Oligonucleotides - chemistry Oligonucleotides - metabolism Oligonucleotides - pharmacology Phosphoric Diester Hydrolases - metabolism Pyrimidines - chemistry |
| Title | Enzymatic hydrolysis and biological activity of oligonucleotides containing 5-substituted pyrimidine bases |
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