Nucleic acid-targeted antimicrobial therapy is a groundbreaking advancement in the field of infectious disease therapeutics. At Protheragen, we provide extensive preclinical development services for nucleic acid-targeted antimicrobial therapies. Our team of seasoned scientists and researchers utilizes state-of-the-art technologies and innovative methodologies to design, refine, and assess nucleic acid-based treatments targeting a diverse array of pathogens.
Overview of Nucleic Acid-targeted Antimicrobial Therapy
Nucleic acid-targeted antimicrobial therapy is a revolutionary strategy in combating infectious diseases. It harnesses the unique specificity and adaptability of nucleic acids to precisely target and disrupt critical biological processes within microbial pathogens. Unlike conventional antibiotics, which often have broad-spectrum effects on cellular functions, nucleic acid-targeted therapies provide pinpoint accuracy in inhibiting microbial gene expression or essential pathways. This targeted approach enables effective treatment of infections caused by a wide range of pathogens, including bacteria and viruses, offering a superior alternative to traditional therapeutic methods.
Fig.1 Schematic diagram of the use of oligonucleotides to treat bacterial infections. (Moreira L., et al., 2024)
Development of Nucleic Acid-targeted Antimicrobial Therapy
The development of nucleic acid-targeted antimicrobial therapies is an area of intense research and innovation. Advances in molecular biology, bioinformatics, and nanotechnology have significantly propelled this field forward. Recent studies have demonstrated the potential of these therapies to combat a wide range of pathogens, including multidrug-resistant bacteria and emerging viral threats.
- Antisense Oligonucleotides (ASOs): ASOs are short synthetic nucleic acids that bind to complementary mRNA or DNA in microbial cells, inhibiting protein translation or viral replication. They target unique sequences in pathogens, reducing off-target effects and resistance risk.
- DNAzymes: DNAzymes are catalytic DNA molecules that cleave specific RNA sequences, disabling microbial transcripts. They target key RNA involved in metabolism or virulence, showing potential as antimicrobial agents.
- Aptamers: Aptamers are single-stranded DNA or RNA molecules selected via SELEX, with high affinity for microbial targets like proteins or toxins. They can inhibit bacterial function or attachment and can be combined with other agents to enhance antimicrobial efficacy.
Table 1. Representative drugs targeting nucleic acid synthesis in the therapeutic of infectious diseases.
| Drug |
Target Pathogen |
Mechanism of Action |
Description |
Stage |
| Remdesivir |
SARS-CoV, SARS-CoV-2, MERS-CoV |
Inhibits viral RNA-dependent RNA polymerase (RdRp) by acting as a chain terminator. |
High binding affinity to RdRp, causing premature termination of RNA synthesis. |
Approved |
| Ribavirin |
HCV, RSV, SARS-CoV, Influenza |
Inhibits viral RNA polymerase and induces lethal mutagenesis. |
Acts by multiple mechanisms, including IMPDH inhibition and immune modulation. |
Approved |
| Acyclovir |
HSV, VZV |
Inhibits viral DNA polymerase by competitive inhibition. |
Requires phosphorylation by viral thymidine kinase. |
Approved |
| Ganciclovir |
CMV |
Inhibits viral DNA polymerase by acting as a chain terminator. |
Requires phosphorylation by viral thymidine kinase. |
Approved |
| Penciclovir |
HSV, VZV |
Inhibits viral DNA polymerase by competitive inhibition. |
Requires phosphorylation by viral thymidine kinase. |
Approved |
| Tenofovir Disoproxil Fumarate |
HIV, HBV |
Inhibits viral DNA polymerase by acting as a chain terminator. |
High stability due to the phosphonate bond. |
Approved |
| Sofosbuvir |
HCV |
Inhibits viral RNA-dependent RNA polymerase (NS5B) by chain termination. |
High selectivity for viral polymerase. |
Approved |
| Lamivudine |
HIV, HBV |
Inhibits viral reverse transcriptase by chain termination. |
Effective against both HIV and HBV. |
Approved |
| Emtricitabine |
HIV, HBV |
Inhibits viral reverse transcriptase by chain termination. |
Effective against both HIV and HBV. |
Approved |
| Abacavir |
HIV |
Inhibits viral reverse transcriptase by chain termination. |
Effective against HIV. |
Approved |
Disclaimer: Protheragen focuses on providing preclinical research services. This table is for information exchange purposes only. This table is not a treatment plan recommendation. For guidance on treatment options, please visit a regular hospital.
Our Services
At Protheragen, we specialize in providing comprehensive preclinical development services for nucleic acid-targeted antimicrobial therapies. Our expertise spans the entire spectrum of drug development, from target identification and validation to formulation and in vivo testing. We leverage cutting-edge technologies and robust scientific methodologies to accelerate the translation of innovative nucleic acid-based therapies from the laboratory to the clinic.
Workflow of Nucleic Acid-targeted Antimicrobial Therapy Development
Target Identification and Validation
Our team of scientists utilizes cutting-edge genomic and bioinformatics tools to meticulously identify and validate nucleic acid targets that are crucial for microbial survival or virulence. By analyzing the genetic sequences of pathogens and pinpointing unique or conserved regions, we can design nucleic acid molecules that specifically target these sequences. This highly targeted approach ensures exceptional specificity and efficacy, significantly reducing the risk of resistance development.
Drug Design and Optimization
Protheragen's expertise in nucleic acid chemistry empowers us to design and synthesize a diverse array of nucleic acid-based therapeutic agents, including antisense oligonucleotides, DNAzymes, and aptamers. We employ state-of-the-art techniques to introduce chemical modifications that enhance stability, binding affinity, and cellular uptake. Our iterative design and optimization process ensures that each therapeutic agent is meticulously tailored to achieve maximum efficacy and safety.
Formulation and Delivery Systems
Effective delivery systems are a cornerstone of nucleic acid-targeted antimicrobial therapy. Protheragen excels in formulating nucleic acid molecules with advanced delivery platforms, such as lipid nanoparticles, polymeric nanoparticles, and antibody-drug conjugates. These delivery systems enhance the stability and bioavailability of nucleic acid-based therapies, ensuring efficient delivery to the site of infection. Our comprehensive formulation services include optimization of particle size, surface charge, and targeting ligands to maximize therapeutic efficacy.
Preclinical Research
Our preclinical development services encompass rigorous in vitro and in vivo testing to thoroughly evaluate the efficacy, safety, and pharmacokinetics of nucleic acid-targeted antimicrobial therapies. Our state-of-the-art laboratories are equipped with advanced instrumentation for conducting antimicrobial assays, cytotoxicity studies, and pharmacokinetic analyses. Additionally, we conduct comprehensive in vivo studies in relevant animal models to assess the therapeutic potential and safety profile of our nucleic acid-based therapies. These studies provide essential data to support the advancement of these therapies into clinical trials.
Types of Nucleic Acid-targeted Antimicrobial Therapies
Each of these types offers distinct advantages and faces unique developmental challenges, but collectively, they represent a powerful and highly specific arsenal in the ongoing battle against antimicrobial resistance, a challenge Protheragen is dedicated to addressing through advanced scientific innovation. If you are interested in our services, please feel free to contact us.
Reference
- Moreira, Luís, et al. "Promising strategies employing nucleic acids as antimicrobial drugs." Molecular Therapy-Nucleic Acids 35.1 (2024).
All of our services and products are intended for preclinical research use
only and cannot be used to diagnose, treat or manage patients.
