Kinetics of phosphorothioate oligonucleotide metabolism in biological fluids
نویسندگان
چکیده
منابع مشابه
Kinetics of phosphorothioate oligonucleotide metabolism in biological fluids.
The in vitro stability and metabolism of GEM[91, a 25mer phosphorothioate antisense oligonucleotide complementary to the gag mRNA region of HIV-1, was investigated using capillary electrophoresis (CE). The in vitro degradation of the parent compound at 37 degrees C was followed over the course of 120 h in human plasma. A CE method using laser-induced fluorescence detection was able to detect 5'...
متن کاملSynthesis of phosphorothioate-methylphosphonate oligonucleotide co-polymers.
We describe the synthesis and characterization of novel phosphorothioate-methylphosphonate backbone-modified oligodeoxynucleotide co-polymers. These may have potential use as antisense constructs.
متن کاملIn vivo distribution and metabolism of a phosphorothioate oligonucleotide within rat liver after intravenous administration.
In the rat, the liver represents a major site of phosphorothioate oligodeoxynucleotide deposition after i.v. administration. For this reason, we examined the intracellular fate of ISIS 1082, a 21-base heterosequence phosphorothioate oligodeoxynucleotide, isolated from parenchymal and nonparenchymal cell types after systemic dosing using established perfusion and separation techniques followed b...
متن کاملEnzyme kinetics of GTI-2040, a phosphorothioate oligonucleotide targeting ribonucleotide reductase.
Enzyme kinetics of GTI-2040 (5'-GGC TAA ATC GCT CCA CCA AG-3'), a phosphorothioate ribonucleotide reductase antisense, were investigated for the first time in 3' exonuclease solution and human liver microsomes (HLMs), using the ion-pair high-performance liquid chromatogram method for quantification of the parent drug and two major 3'N-1 and 3'N-2 metabolites. Enzyme kinetics of GTI-2040 in 3'-e...
متن کاملMechanisms of a phosphorothioate oligonucleotide delivery by skin electroporation.
Skin electroporation has great potential for topical delivery of oligonucleotides. Controled therapeutic levels of an intact phosphorothioate oligonucleotide (PS) can be reached in the viable tissue of the skin. The aim of this work was to investigate the transport mechanisms of a PS in hairless rat skin by electroporation, and hence to allow optimization of oligonucleotides (ONs) topical deliv...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Nucleic Acids Research
سال: 1997
ISSN: 0305-1048,1362-4962
DOI: 10.1093/nar/25.18.3615