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siRNA Amino Acid Modification

Small interfering RNA (siRNA) therapies are revolutionizing precision medicine, yet their efficacy hinges on overcoming delivery and stability challenges. At Protheragen BioNucleics, we specialize in siRNA amino acid modification, a cutting-edge approach to enhance oligonucleotide performance. Our expertise spans Oligonucleotide Drugs CRO, Oligonucleotide Modification Service, and siRNA Modification Service, enabling tailored solutions for therapeutic development. By integrating amino acid modifications into siRNA scaffolds, we bridge the gap between lab-scale innovation and and preclinical.

Overview of siRNA Amino Acid Modification

siRNA amino acid modification involves the strategic incorporation of amino acid residues or side chains into siRNA molecules. Unlike traditional chemical modifications (e.g., phosphorothioate backbones or 2'-O-methyl sugars), amino acid conjugation enhances siRNA functionality through:

Improved biodistribution: Amino acids enable receptor-specific targeting.
Enhanced stability: Resistance to nucleases and serum degradation.
Reduced immunogenicity: Natural amino acids minimize immune recognition.

This approach allows precise control over siRNA interactions with biological systems, making it ideal for in vivo applications. Our team optimizes modifications to balance potency, safety, and manufacturability.

Core Services in siRNA Amino Acid Modification

Protheragen BioNucleics offers end-to-end solutions for siRNA amino acid modification, leveraging proprietary technologies to meet diverse therapeutic goals:

Design & Sequence Optimization

We utilize AI-driven algorithms to predict optimal amino acid insertion sites, ensuring minimal interference with siRNA's gene-silencing activity. Our platform evaluates thermodynamic stability, off-target effects, and binding affinity to refine sequences for in vivo efficacy.

Site-Specific Conjugation

Using click chemistry, NHS esters, or maleimide-thiol reactions, we conjugate amino acids (e.g., lysine, arginine) to siRNA strands. This precision ensures reproducible attachment at predefined positions (e.g., sense strand 3'-end), enhancing tissue targeting without compromising RNA-induced silencing complex (RISC) loading.

Functional Group Engineering

We modify amino acid side chains to introduce functionalities such as:

PEGylation: Prolongs circulation half-life.
Lipidation: Improves cellular uptake via membrane fusion.
Ligand attachment: Enables active targeting (e.g., galactose for hepatocyte-specific delivery).

Stability & Efficacy Profiling

Our in vitro / in vivo assays assess:

Serum stability (via HPLC).
Gene silencing efficiency (qRT-PCR).
Toxicity and immunogenicity (cytokine profiling).

Formulation Support

We develop lipid nanoparticles (LNPs) or polymer-based carriers to protect modified siRNAs during systemic delivery, prioritizing scalability for GMP production.

Customized Modifications

Clients access bespoke services, including:

Non-canonical amino acid incorporation.
Multi-arm conjugates for multivalent targeting.
Hybrid modifications combine amino acids with sugars or lipids.

Frequently Asked Questions

Q1: How do amino acid modifications differ from other siRNA stabilization methods?

Amino acids enhance both stability and targeting via natural biochemical interactions, unlike passive stabilization (e.g., 2'-O-methyl). They also reduce toxicity risks associated with synthetic polymers.

Q2: Can these modifications improve siRNA delivery to non-liver tissues?

Yes. Conjugating tissue-homing peptides (e.g., RGD for tumors) or antibodies enables extrahepatic targeting, broadening therapeutic applications.

Applications of siRNA Amino Acid Modification

Oncology

Tumor-specific siRNAs with peptide ligands.

Genetic Disorders

Enhanced CNS delivery for neurodegenerative diseases.

Antiviral Therapies

Stabilized siRNAs against RNA viruses.

Metabolic Diseases

Liver-targeted conjugates for dyslipidemia.

Why Partner with Us?

Proprietary AI Tools: Accelerate design and reduce trial cycles.
End-to-End Expertise: From concept to preclinical validation.
Collaborative Approach: Co-development models to align with client goals.

Our services and products are exclusively for authorized organizations in research, development, or manufacturing and are not intended for direct use by individuals or patients or as medical advice, diagnosis, or treatment.