Link Technologies Ltd has expanded its range of lipophilic modifiers for the effective delivery of oligonucleotides into cells. As oligos continue to be of interest in drug discovery, offering exciting potential as therapeutic agents, there is an increasing demand for improved oligo delivery techniques.
Link’s proven collection of lipophilic oligo modification reagents, which include cholesterol and tocopherol modifiers, now also includes 5’-Palmitate-C6-CE Phosphoramidite.
As a derivative of palmitic acid, a physiologically common fatty acid, the new palmitate modifier is the first palmitate phosphoramidite available commercially, and provides scientists with an ideal approach to improve the cellular uptake and utilization of oligos.
In the cell, palmitic acid is known to conjugate to proteins via cysteine residues and, in doing so, is believed to aid the movement of proteins between intracellular compartments. It is also known that improved cell delivery is achieved when an oligonucleotide is modified with palmitic acid, and that modification at the 5’-end results in more efficient uptake than modification at the 3’-end.
However, until now, modification of the 5’-end of the oligo with palmitic acid has proved inefficient. For this reason, Link has developed 5’-Palmitate-C6-CE Phosphoramidite, the first of its palmitic acid derived phosphoramidites, as a dedicated delivery reagent.
When incorporated during oligo synthesis, the use of this novel palmitate modifier can result in more efficient uptake of the oligonucleotide by the cell, offering important value particularly for therapeutic applications.
Commenting on the new addition to Link’s breakthrough range of lipophilic modifiers, Catherine McKeen, Head of Technology Commercialisation, explained: “Labelling oligos with hydrophobic compounds has proved a successful technique for enhancing cell delivery. We are continuing to develop our range of reagents for use in this field so that we can always offer our customers the most effective methods for oligo delivery. Palmitate, due to its proven ability to improve oligonucleotide delivery, is a natural choice for addition to our delivery agent portfolio.”