Resistance of Morpholino Phosphorodiamidate Oligomers to Enzymatic Degradation
- 1 January 1996
- journal article
- research article
- Published by Mary Ann Liebert Inc in Antisense and Nucleic Acid Drug Development
- Vol. 6 (4) , 267-272
- https://doi.org/10.1089/oli.1.1996.6.267
Abstract
Oligomers possessing the Morpholino phosphorodiamidate backbone were evaluated for resistance to a variety of enzymes and biologic fluids. A 25-mer was incubated with nucleases, proteases, esterases, and serum, and the reaction mixtures were directly analyzed by MALDI-TOF mass spectrometry. The 25-mer was completely resistant to 13 different hydrolases and serum and plasma. The excellent resistance of the Morpholino phosphorodiamidates to enzymatic attack indicates their suitability for in vivo use.Keywords
This publication has 7 references indexed in Scilit:
- Efficacy of Morpholino-modified Antisense Oligomers Directed against Tumor Necrosis Factor-α mRNAPublished by Elsevier ,1996
- A Simple Method for Delivering Morpholino Antisense Oligos into the Cytoplasm of CellsAntisense and Nucleic Acid Drug Development, 1996
- Stability measurements of antisense oligonucleotides by capillary gel electrophoresisJournal of Chromatography A, 1995
- Interactions of oligonucleotide analogs containing methylphosphonate internucleotide linkages and 2′-O-methylribonucleosidesNucleic Acids Research, 1994
- Comparative evaluation of seven oligonucleotide analogs as potential antisense agentsJournal of Medicinal Chemistry, 1993
- Oligothymidylate analogues having stereoregular, alternating methylphosphonate/phosphodiester backbones. Synthesis and physical studies.Journal of Biological Chemistry, 1980
- 399. Phosphoramidic halides: phosphorylating agents derived from morpholineJournal of the Chemical Society, 1958