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RNA interference (RNAi) is a cellular mechanism that inhibits gene expression by suppressing its transcription or activating the RNA degradation process. The mechanism was discovered by Andrew Fire and Craig Mello in 1998 in plants. Today, it is observed in almost all eukaryotes, including protozoa, flies, nematodes, insects, parasites, and mammals. This precise cellular mechanism of gene silencing has been developed into a technique that provides an efficient way to identify and determine the...
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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Related Experiment Video

Updated: Apr 24, 2026

Sequence-specific and Selective Recognition of Double-stranded RNAs over Single-stranded RNAs by Chemically Modified Peptide Nucleic Acids
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Antisense oligonucleotides in cancer.

Daniela Castanotto1, Cy A Stein

  • 1Department of Medical Oncology and Experimental Therapeutics, City of Hope, Duarte, California, USA.

Current Opinion in Oncology
|September 5, 2014
PubMed
Summary

Antisense oligonucleotide cancer therapy has not succeeded due to poor delivery and cellular uptake. Further research into pharmacology and delivery is needed for clinical success.

Area of Science:

  • Molecular Biology
  • Pharmacology
  • Oncology

Background:

  • Antisense oligonucleotide (ASO) therapy has long promised to silence cancer-causing genes.
  • Despite decades of research, ASO-based cancer treatments have not reached clinical success.

Purpose of the Study:

  • To review the reasons for the lack of success in ASO cancer therapy.
  • To identify barriers hindering the clinical application of ASO therapy for cancer.

Main Methods:

  • Review of scientific literature on ASO design, delivery, and clinical trials.
  • Analysis of chemical modifications and their impact on oligonucleotide properties.
  • Discussion of phase III clinical trial data for ASO cancer indications.

Main Results:

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  • Significant advancements in ASO chemical modifications have improved absorption, distribution, metabolism, and reduced toxicity.
  • Despite improvements, ASO delivery and cellular uptake remain insufficient for therapeutic efficacy.
  • Phase III trials for ASO cancer indications have not yet led to marketed therapies.

Conclusions:

  • No antisense oligonucleotide is currently marketed for cancer treatment.
  • Critical aspects of ASO cellular pharmacology and delivery in tumors are not yet fully understood.
  • Further investigation into these areas is essential for realizing the potential of ASO cancer therapy.