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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Bibliographic Details
Published inNucleosides & nucleotides Vol. 18; no. 6-7; pp. 1665 - 1666
Main Authors Otvös, L, Sági, J, Sági, G, Szemzõ, A, Tóth, F D, Jeney, A
Format Journal Article
LanguageEnglish
Published United States 01.06.1999
Subjects
Blood
Humans
Hydrolysis
Kinetics
Oligonucleotides - chemistry
Oligonucleotides - metabolism
Oligonucleotides - pharmacology
Phosphoric Diester Hydrolases - metabolism
Pyrimidines - chemistry
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Summary: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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0732-8311
DOI:10.1080/07328319908044816