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CpG-siRNA Conjugate Development

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CD Formulation is at the forefront of innovation in drug delivery, focusing on the optimization of CpG-siRNA conjugates to offer superior solutions for our clients. Furthermore, we are committed to revolutionizing vector design to enhance stability and delivery efficiency in vivo, thereby providing our customers with a more competitive product support and service experience.

Why Customize CpG-siRNA Conjugates?

CpG ODNs linked with Dicer substrate siRNA are identifiable by TLR9-expressing cells in both humans and mice. These complexes efficiently target and suppress gene expression in mouse TLR9+ immune cells, like dendritic cells (DCs), macrophages, and B cells, in vitro and in vivo, without the necessity for transfection agents. Efficacy studies in mice have demonstrated that CpG can directly and/or immune-mediatedly target various tumorigenic factors via siRNA, including the anti-tumorigenic activities of STAT3, STAT5, RELA/P65, BCL2L1, and S1PR1. In summary, CpG-siRNA conjugates offer several advantages:

Overcoming the limitations of small molecule drugs.
Eliminate the necessity for intricate formulations or delivery systems.
Enable dual targeting of cancer cells and immune cells to enhance treatment efficacy.

Explore Our CpG-siRNA Conjugate Development Services

Customization Services for CpG-siRNA Conjugates

The CpG-siRNA conjugate custom development service is designed to offer researchers efficient and specific solutions for gene silencing. This service encompasses various components, including the design and synthesis of siRNA sequences targeting specific genes, modification of CpG structures, purification, and functional evaluation.

CpG-siRNA Conjugate Optimization Service

CpG Modification Services	SiRNA Modification Services
Enhancing the immunostimulatory effects of CpG oligonucleotides involves sequence modifications. These optimization services include the assessment of CpG sequence immunogenicity and conservation analysis across multiple species. Also, chemical modifications can be employed to improve stability and minimize potential immune side effects.	The modification of small interfering RNAs (siRNAs) involves optimizing the sequence combinations to enhance their efficacy in specific cell types. Chemical modifications, including phosphate backbones, end protection, and base alterations, can significantly improve the stability and cytocompatibility of siRNAs, thereby extending their duration of action.

Binding Agent Development

We are concentrating on optimizing binding methods for CpG-siRNA conjugates by developing innovative binding agents to enhance their stability and specificity. Our team of experts is committed to researching and designing efficient binding agents to ensure reliable performance across various biological environments.

Drug Delivery Carriers Development

We are developing novel and efficient vector systems to enhance the delivery efficiency of CpG-siRNA conjugates. Our goal is to achieve improved cell targeting and drug delivery efficiency through advanced vector technologies. These vectors not only exhibit excellent biocompatibility but also minimize side effects, providing a robust technical foundation for clinical applications. We look forward to delivering significant value enhancement to our customers' scientific research and product development through these efforts.

General Workflow for Process of CpG-siRNA Conjugates Development

Fig.1 Workflow for CpG-siRNA conjugates development. Fig.1 Flow chart of CpG-siRNA conjugate development. (CD Formulation)

Program Development

Our scientific team develops detailed and customized experimental protocols, including the design of CpG oligonucleotide and siRNA sequences, tailored to meet customer needs.

Synthesis and Modification

CpG and siRNA are chemically synthesized according to their design and may be chemically modified, if necessary, to enhance stability and delivery efficiency.

Conjugate Construction

The synthesized CpG and siRNA are combined using appropriate chemical methods or structural designs to form CpG-siRNA conjugates.

Quality Control

Perform various quality tests on the product, including purity tests, structural confirmation, and biological activity assays, to ensure that it meets the required standards.

Experimental Validation

Validate the efficacy and safety of CpG-siRNA conjugates using appropriate in vitro or in vivo models, and conduct functional tests.

Data Analysis and Reporting

Analyze experimental data and provide comprehensive study reports along with follow-up recommendations. This includes data interpretation and optimization protocols.

Our Technology Platforms

Synthesis Platforms

Items	Descriptions
Solid-Phase Synthesis	This method employs a solid support to synthesize oligonucleotides and is commonly used for the preparation of CpG sequences.
Enzymatic Synthesis	Precise ligation and modification of nucleic acids through enzymatic catalysis.

Analytical Platforms

Items	Descriptions
NMR Platform	NMR technology to determine molecular structures and interactions.
HPLC Platform	HPLC is utilized for purity and component analysis to ensure the quality and consistency of synthetic compounds.

Advantages of Our CpG-siRNA Conjugate Development Services

Conjugate design can enhance the stability of siRNA in vivo, prolong its half-life, and improve the efficacy and durability of the drug.
With optimized chemical modifications and nanocarriers, CpG-siRNA conjugates can be efficiently delivered to the target site, ensuring the precise entry of siRNA into target cells.
Development services offer customized conjugate design tailored to meet the specific needs of various research and therapeutic programs.
With professional development technologies and platforms, we can promote cutting-edge scientific research and provide strong support for new drug development and basic research.

Published Data

Technology: CpG oligonucleotides conjugated with siRNA using chemical synthesis technology

Journal: The Journal of the American Society of Hematology

IF: 21.0

Published: 2013

Results:

STAT3 is crucial in cancer and immune cells, aiding cancer progression but challenging for drug targeting. Using TLR9 agonists like CpG oligonucleotides, researchers achieve targeted siRNA delivery in mouse immune cells, and now show similar results in human TLR9+ hematopoietic cells. They developed CpG(A)-STAT3 siRNA conjugates, effectively silencing genes and activating immune cells like dendritic and B cells in vitro. TLR9 is present in diseases like B-cell lymphoma and leukemia. The study demonstrates CpG(A)-siRNAs can knock down proteins like STAT3 and BCL-XL in TLR9+ tumor cells, inhibiting tumor growth. These siRNAs are safe for normal leukocytes and could be a promising dual-action therapy for blood cancers.

Fig.2 CpG-siRNA in TLR9+ MM/AML cells. Fig.2 CpG-siRNA uptake and gene silencing in TLR9+ MM and AML cells. (Zhang Q, et al., 2013)

CD Formulation is committed to providing you with state-of-the-art CpG-siRNA conjugate development services to meet your research needs. If you have any questions or need further information, please feel free to contact us.

References

Zhang Q, Hossain D M S, Nechaev S, et al. TLR9-mediated siRNA delivery for targeting of normal and malignant human hematopoietic cells in vivo. Blood, The Journal of the American Society of Hematology, 2013, 121(8): 1304-1315.

How It Works

STEP 1

Submit a service request describing your specific research or development need.

STEP 2

We'll email you to provide your quote and confirm order details if applicable.

STEP 3

Execute the project with real-time communication, and deliver the final report promptly.

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