Oligonucleotide therapeutics are rapidly becoming a major focus in modern drug development. Unlike traditional small molecules or antibody drugs, these therapies directly regulate gene expression at the RNA level through sequence-specific targeting of mRNA.

Because of their high specificity, strong efficacy, and broad therapeutic potential, oligonucleotide drugs are attracting growing interest in areas such as cardiovascular disease, genetic disorders, oncology, and neurological diseases.

A major breakthrough came with the FDA approval of Leqvio, the long-acting siRNA therapy co-developed by Novartis and Alnylam Pharmaceuticals. Its success further accelerated global investment in RNA therapeutics and oligonucleotide drug discovery. 

Major Types of Oligonucleotide Therapeutics

The main categories of oligonucleotide drugs include:

  • ASO (Antisense Oligonucleotides) — regulate or degrade target mRNA
  • siRNA — induce RNA interference-mediated mRNA cleavage
  • miRNA — restore or modulate endogenous RNA regulation
  • Aptamers — bind target proteins with high specificity

Each type offers unique advantages in specificity, delivery, potency, and therapeutic applications. 

Oligonucleotide Drug Development Workflow

The development of oligonucleotide therapeutics is a multi-stage process that typically encompasses disease indication selection, target identification, sequence design, chemical modification, delivery optimization, and process development and manufacturing.

Among these steps, identifying highly effective and sequence-specific candidate molecules is critical for successful drug development.

Because oligonucleotide therapeutics act directly on intracellular RNA, RT-qPCR-based RNA expression analysis has become one of the most important tools for evaluating candidate efficacy.

Figure 1. Oligonucleotide Drug Development Workflow

Figure 1. Oligonucleotide Drug Development Workflow

Integrated RNA Screening Solution for Oligonucleotide Drug Discovery

To support high-throughput oligonucleotide screening workflows, Yeasen Biotechnology provides a comprehensive solution combining automated RNA extraction with highly sensitive RT-qPCR detection platforms.

This workflow enables researchers to rapidly evaluate RNA-level changes in candidate-treated samples with high sensitivity, reproducibility, and throughput.

Using one-step RT-qPCR kits, highly expressed targets could be detected down to 0.1 pg RNA input, while moderately expressed targets were detectable at 1 pg levels.

  • Hifair™ Advanced One Step RT-qPCR SYBR Green Kit(Cat#11175)

This one-step SYBR Green I kit combines RT and qPCR in a single tube to maximize efficiency and minimize contamination. Powered by Hifair™ V Reverse Transcriptase and HotStart Taq DNA Polymerase, it achieves high sensitivity for RNA samples, detecting as low as 0.1 pg for highly expressed targets and 1 pg for moderately expressed targets. It also supports DNA quantification across diverse animal, plant, cell, and microbial samples.

Figure 2: Quantitative results of the one-step RT-qPCR SYBR Green Kit

Figure 2: Quantitative results of the one-step RT-qPCR SYBR Green Kit

When tested with RNA samples, the results demonstrated that the kit can detect targets at the 0.1 pg level for highly expressed genes and at the 1 pg level for moderately expressed genes.

  • Hieff™ Advanced Fast One Step RT-qPCR Probe Mix (Cat#16949)

Designed for rapid one-step RT-qPCR directly from cell lysates, this reagent combines RT and qPCR in a single tube to reduce reaction time and contamination risk. Featuring high tolerance and broad compatibility, it is ideal for high-throughput expression analysis in 96- or 384-well plates. The 100T format covers two 96-well plates to prevent freeze-thaw degradation, while the 500T format is optimized for automated 384-well screening platforms.

Figure 3. Superior Multiplex Amplification Capability

Figure 3. Superior Multiplex Amplification Capability

Using the same cell samples, cell lysis and one-step RT-qPCR amplification were performed using Cat#16949 and Supplier T*. The results demonstrate that Cat#16949 exhibits superior peak profiles and a higher detection rate for individual targets within the multiplex amplification system.

As RNA therapeutics continue to reshape precision medicine, efficient RNA screening technologies are becoming increasingly important for candidate discovery and validation.

By integrating automated RNA extraction with sensitive RT-qPCR analysis, researchers can accelerate oligonucleotide drug development with improved efficiency, reproducibility, and confidence.

Related Products

Category

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Cat. No.

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96-Channel Automated Nucleic Acid Extractor

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Direct RT-qPCR (Dye-Based Method)

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Hieff™ Fast Cell Direct SYBR Green RT-qPCR Kit

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Direct RT-qPCR (Probe-Based)

Hieff™ Fast Cell Direct Probe RT-qPCR Kit

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Hieff™ Fast Cells Lysis Kit

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Hieff™ Advanced Fast One Step RT-qPCR Probe Mix

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Hieff™ Fast Cells-to-CT One Step RT-qPCR Probe Mix

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