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https://www.ncbi.nlm.nih.gov/pubmed/19530907
Nonetheless, the first studies on the oral delivery of siRNA in animals and antisense oligonucleotides in humans suggest that significant oral delivery of these nucleic acids can be achieved across the gut wall.Author: Saghir Akhtar
https://www.tandfonline.com/doi/abs/10.1080/10611860903057674
Apr 21, 2009 · Inhibition of gene expression with antisense oligonucleotides or RNA interference (RNAi) mediated gene silencing by small interfering RNA (siRNA) has tremendous potential to silence the expression of disease-causing genes in the clinic. A major hurdle to their widespread clinical use is the safe and efficient delivery to target cells in vivo. Delivery via the oral route is considered the holy grail for small molecule and macromolecular drug delivery …Author: Saghir Akhtar
https://www.researchgate.net/publication/26296131_Oral_delivery_of_siRNA_and_antisense_oligonucleotides
Nonetheless, the first studies on the oral delivery of siRNA in animals and antisense oligonucleotides in humans suggest that significant oral delivery of these nucleic acids can be achieved across...Author: Saeed Akhtar
https://www.sciencedirect.com/science/article/pii/S0168365912005378
Small interfering RNA (siRNA), microRNA (miRNA), antisense oligonucleotides (AS-ODNs), and transcription factor decoys are oligonucleotides that can regulate gene expression when delivered to the cytosol . These four strategies all use a short sequence of nucleotides (approximately 20 base pairs), and each strategy requires intracellular delivery and endosomal escape of the oligonucleotides.Author: Diane C. Forbes, Nicholas A. Peppas
https://www.sciencedirect.com/science/article/abs/pii/S0168365912005378
The promise of short RNA or DNA segments such as siRNAs, antisense oligonucleotides, and transcription factor decoys to treat disease has prompted nearly 40 clinical trials for RNA interference (RNAi)-based therapeutics and more than 100 clinical trials for antisense oligonucleotide-based technologies; in fact, there are promising in vivo and preclinical studies for many hundreds of …
https://www.sciencedirect.com/science/article/pii/S0022354916324522
Oral absorption of the 2′‐O‐(2‐methoxyethyl) modified antisense oligonucleotide (2′‐MOE ASO), ISIS 104838, was demonstrated in healthy volunteers with an average 9.5% plasma bioavailability across four formulations tested. The greatest average performance achieved in this study for a single formulation was 12.0% bioavailability within an individual dose and subject range of 1.96–27.5%.Author: Lloyd G. Tillman, Richard S. Geary, Gregory E. Hardee
https://www.sciencedirect.com/science/article/pii/S0168365908006834
Mar 04, 2009 · Small interfering RNAs (siRNA) are typically ~ 23 bp in length and utilize a cell's own RNA interference pathways to catalyze the degradation of targeted mRNA transcripts , whereas antisense oligonucleotides (AON) are single-stranded and can act additionally by altering splicing of pre-mRNA . While many diseases might be approached by direct knockdown, at least one disease that now …
https://www.sigmaaldrich.com/catalog/papers/17721945
Oral delivery of antisense oligonucleotides in man. Treatment of systemic disease with phosphorothioate antisense oligonucleotides (PS ASOs) has been accomplished using local or parenteral routes of administration to date.
https://www.sciencedirect.com/science/article/pii/S0378517308004468
8. Polymeric nanoparticles for the delivery of antisense oligonucleotides and siRNA. Despite the continuous synthesis of new entities of AS-ODNs or more recently siRNA, a few issues remain to be solved to optimize their delivery.
https://www.cell.com/molecular-therapy-family/nucleic-acids/pdf/S2162-2531(16)30083-X.pdf
Delivery of Antisense Oligonucleotides Järver et al 2 initiation or elongation and thus decrease the levels of the cor-responding protein (Figure 1a). Steric blocking of ribosomal elongation is known to be hard to achieve, but blocking of ribo-somal initiation can be efficient by targeting the initiator AUG
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