Conjugates

Conjugation of Morpholino oligos with endosomal escape moieties is bringing effective antisense techniques to rodent research. Such conjugates will likely debut soon as therapeutics. This is an open-access review of two delivery-enabled forms of Morpholinos. Moulton JD, Jiang S. Gene Knockdowns ...

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... Proc Natl Acad Sci U S A. 2009 Jan 27;106(4):1205-10. Epub 2009 Jan 21. Moulton HM, Moulton JD. Antisense Morpholino Oligomers and Their Peptide Conjugates. In: Therapeutic Oligonucleotides, edited by Jens Kurreck, Royal Society of Chemistry 2008.

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... Of course, without clinical trial data we cannot make certain statements about the efficacy of the Morpholino-peptide conjugates in human systems. But they work in other mammals, as discussed in the publications I cited previously. Another option for in-vivo delivery ...

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... 4; [Epub ahead of print] Lebleu B, Moulton HM, Abes R, Ivanova GD, Abes S, Stein DA, Iversen PL, Arzumanov AA, Gait MJ. Cell penetrating peptide conjugates of steric block oligonucleotides. Adv Drug Deliv Rev. 2008 Mar 1;60(4-5):517-29. Epub 2007 Oct 22. Lai SH, Stein DA, Guerrero-Plata A, Liao ...

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... Delivery of Morpholino Antisense Oligo. Bioconjug Chem. 2008 Jul;19(7):1464-70. Epub 2008 Jun 20. Studies on the arginine-rich peptide-Morpholino conjugates have shown that the oligos enter cells by endocytosis and then escape from the endosome. In some way, the peptide moieties render the endosomal ...

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