PNA-lipophilic Ligand Conjugates Synthesis

PNA-lipophilic Ligand Conjugates Synthesis

About PNA-lipophilic Ligand Conjugates

Lipophilic ligands are a class of substances suitable for cell transport, they are lipids with a certain hydrophilic-lipophilic balance. When transported across the cell membrane, the hydrophilic end faces the extracellular water-soluble environment, and the hydrophobic end faces the cell membrane. A typical representative of this modification is the covalent attachment of bile acid and cholesterol to PNA. The conjugate also has a certain liver-targeting effect in vivo and has the potential to develop into a liver-targeted preparation.

Synthesis Examples

Some lipophilic ligand compounds have been successfully used for PNA transport.


Conjugation strategy

Target cell type

Cholic acidPNA-cholic acid-ester hemisuccinateHeLa pLuc705
CholesterolPNA-cholesterol-ester hemisuccinateHeLa pLuc705
HeteroaromatPNA-heteroaromatHeLa pLuc705; p53R
OligophosphonatePNA-(Gln-phosphonate)m PNA-(Lys-bis-phosphonate)nHeLa pLuc705


PNA-lipophilic Ligand Conjugates Synthesis

The covalent binding of PNA with hydrophobic compounds or lipids has some excellent properties. For example, by connecting a hydrophobic long carbon chain to the N-terminus of PNA and amino acid residues to the C-terminus, the conjugate has good hydrophilicity and lipophilicity, and shows better specificity when hybridizing with DNA. The conjugate can also self-assemble into spherical micelles, and has application potential in biosensors, gene drugs, etc. PNA-lipophilic ligand conjugate also shows good performance in cell transport.

  • By combining PNA with cholesterol or cholic acid through a hemisuccinate bond, the resulting conjugate can pass through cell membranes efficiently, and the water solubility of the PNA-cholic acid conjugate is better.
  • PNA and cholesterol are connected through lysine, and its transport performance and DNA specific binding performance are very good.
  • Aromatic heterocyclic compounds generally have the function of enhancing PNA transport, and the conjugates formed by acridine and nicotinic acid with PNA have the highest activity.
  • The covalent attachment of polyphosphate to PNA significantly enhances the cell transport of PNA without affecting its hybridization specificity and affinity.
  • PEI can be used as an efficient guide for PNA transfer into cells, and is not affected by intracellular lysosomes.

Our Advantages

  • Multi-strategy

    We will continue to develop new strategies to synthesize new PNA monomers and find new complexes to meet customer needs in the future.

  • Multi-functional

    We are committed to making synthetic products capable of optimizing multiple functions of PNA and improving the quality of products.

  • Multi-application

    Through the new strategy
    and the guarantee of
    product quality, we
    hope that the
    product will be applied
    in many aspects.

Creative Peptides has completed many PNA conjugate synthesis cases. Based on these projects, our team has accumulated a deep understanding of product requirements. With rich experience and scientific knowledge, our experts are dedicated to helping our customers navigate and accelerate your PNA synthesis plan. By combining scientific knowledge and laboratory experience, we are committed to expanding your understanding and applications of PNA conjugates. Please contact us to learn more.


  • Liu C.D., et al.Cellular transport of modified peptide nucleic acids. Chinese Journal of Bioengineering. 2016, 32(3): 292-305.

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