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Related Experiment Video

Updated: Jul 2, 2026

Sequence-specific and Selective Recognition of Double-stranded RNAs over Single-stranded RNAs by Chemically Modified Peptide Nucleic Acids

Sequence-specific and Selective Recognition of Double-stranded RNAs over Single-stranded RNAs by Chemically Modified Peptide Nucleic Acids

Published on: September 21, 2017

An efficient biodelivery system for antisense polyamide nucleic acid (PNA).

Mohamed Mehiri¹, Gregory Upert, Snehlata Tripathi

¹Laboratoire de Chimie des Molécules Bioactives et des Arômes, Université de Nice-Sophia Antipolis-CNRS, Institut de Chimie de Nice, Nice, France.

Oligonucleotides

|August 19, 2008

Summary

Researchers developed a novel triphenylphosphonium (TPP) transporter for delivering peptide nucleic acids (PNAs) into cells. This system effectively releases PNAs in the cytosol, demonstrating significant anti-HIV activity.

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Synthesis, Functionalization, and Characterization of Fusogenic Porous Silicon Nanoparticles for Oligonucleotide Delivery

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Published on: April 16, 2019

Area of Science:

Biotechnology
Molecular Biology
Drug Delivery Systems

Background:

Intracellular delivery of naked nucleic acids like peptide nucleic acids (PNAs) remains a challenge.
Developing efficient and straightforward delivery methods is crucial for therapeutic applications.

Purpose of the Study:

To design a general and straightforward procedure for intracellular delivery of naked PNAs.
To create a biodegradable transporter system for enhanced PNA delivery and efficacy.

Main Methods:

A triphenylphosphonium (TPP) cation-based transporter system was designed, linked via a disulfide bridge to an activated mercaptoethoxycarbonyl moiety.
The TPP-PNA conjugate was synthesized and its stability in cell culture medium and cytosol-mimicking conditions was assessed.
Cellular uptake and intracellular release of PNA were evaluated using fluorescence-labeled conjugates and anti-HIV activity assays.

Main Results:

TPP-PNA-carbamate conjugates showed high stability in cell culture medium but were rapidly degraded in glutathione-containing medium, releasing free PNA.
Fluorescence-labeled conjugates demonstrated efficient cellular uptake.
The TPP-conjugate of a 16-mer PNA targeting HIV-1 TAR region exhibited significant anti-HIV activity (IC50 = 1 microM), unlike the free PNA.

Conclusions:

The developed TPP-based transporter system enables efficient intracellular delivery and release of naked PNAs.
This system offers a promising strategy for enhancing the therapeutic efficacy of PNAs, as evidenced by its anti-HIV activity.