To add to the range of cell delivery modifications we are introducing a pyridoxine (vitamin B6) amidite (2536). The DMT protection allows DMT-ON purification. Pyridoxine has several biological functions: red blood cell production; homocysteine reduction; inflammation reduction and neurotransmitter production. It is known that almost all eukaryotic cells have receptor mediated transport system for this vitamin where pyridoxine acts as a carrier and, once the biomolecule is in the cell or cell compartment, the carrier is lost as pyridoxial phosphate. There is evidence that cellular uptake of peptide-oligonucleotide conjugates has been improved where pyridoxine has been conjugated to the peptide.
Although the vitamin is attached via an amide, an enzymatic conversion takes place and the carrier is still released as the phosphate. This modification allows the direct incorporation at the 5’-end of an oligo and, once in the cell,
it is thought that the carrier will be hydrolysed from the oligo.
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.