5’-Niacin Modified Oligonucleotides and Their Effect on Cellular Uptake

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Link has developed a pyridine based synthesis reagent derived from niacin. This vitamin is important in the biosynthesis of NAD and NADH, hence is recognised by cells. Being much less hydrophobic and bulky than more commonly used delivery reagents it is anticipated the need to remove modifiers derived from niacin will no longer be necessary. Also since these are important in many biological pathways that once in the cell, it is possible that these will be removed by hydrolysis of the phosphate linkage.

Niacin is an essential vitamin and is one of only five where deficiency results in a pandemic deficiency disease, in this case pellagra. It is known for its therapeutic effects as a lipid lowering drug. This works by inhibiting the production of cyclic AMP and as a result the liver is unable to produce LDL. Recently niacin has been shown to improve the ability of immune cells to kill staphylococcus bacteria (responsible for MRSA).

Link has developed a 5’-niacin phosphoramidite (2530) to allow efficient incorporation of niacin to the 5’-end of an oligonucleotide.

Click the link below to download the article. This product is now available to order online. View the use protocol here.

Intellectual Property
Use of 5'-Niacin-CE Phosphoramidite, 5'-Niacin-C6-CE Phosphoramidite and bisDMT-Pyridoxine-C6-CE Phosphoramidite (Patent Pending PCT/GB2015/050611) is only permitted for incorporation into oligonucleotides for private purposes, including Research Use Only (RUO) oligonucleotides, i.e. not for commercial applications. Purchase of these products from LINK allows the purchaser the right to sell an oligonucleotide modified with the products, but only for RUO by the end-user. This right only applies to product purchased from Link Technologies or a licenced vendor. For all other uses of these products, in particular commercial applications, licensing programs are available from Link Technologies Ltd. For the avoidance of doubt, a separate licence must be sought for any synthesis and commercial sale of any oligonucleotide modified with the product for any non-RUO purpose, such as, but not limited to, therapeutic and diagnostic applications. Please contact us for further details.

 

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