Target intelligence / Profile preview

CpG motif–containing DNA, Toll-like receptor 9 agonist (in the context of adjuvant BC02) (CpG ODN (ODN = oligodeoxynucleotide))

Target
CpG ODN (ODN = oligodeoxynucleotide)
Molecular classification
Other (synthetic DNA motif), Pattern recognition receptor ligand (PRR ligand), Adjuvant (vaccine component), Nucleic acid
01

Overview

CpG oligodeoxynucleotide motifs are short, synthetic single-stranded DNA sequences that contain unmethylated cytosine-guanosine dinucleotides and mimic bacterial DNA patterns. These motifs are recognized by Toll-like receptor 9 (TLR9), primarily expressed on plasmacytoid dendritic cells and B cells. Upon binding, CpG ODN triggers signaling pathways (e.g., MyD88, MAPK, NF-κB) leading to the production of proinflammatory cytokines and maturation of antigen-presenting cells, thereby stimulating both humoral and cellular arms of the immune response. BC02 is a compound adjuvant consisting of BCG-derived CpG DNA and aluminum hydroxide, designed to synergistically enhance immune responses to co-administered vaccines, facilitating robust Th1 and Th2 immunity and increased antigen-specific antibody production. CpG-containing adjuvants are used in licensed vaccines (e.g., HEPLISAV-B) and explored for infectious diseases, cancer immunotherapy, and allergy immunotherapy.

Other names
CpG DNACpG ODNunmethylated CpG oligodeoxynucleotidesTLR9 agonistBCG CpG DNABC02 adjuvantCpG-based adjuvant
02

Mechanism of action

Activation of Toll-like receptor 9 (TLR9) on plasmacytoid dendritic cells and B cells; Induction of innate and adaptive immune responses; Enhancement of Th1/Th2 cytokine production; Upregulation of co-stimulatory molecules; Activation of NF-κB and MAPK pathways in immune cells.

03

Biological functions

Immune response activationInduction of Th1 and Th2 immunityUpregulation of cytokinesMaturation of dendritic cellsB cell activation and antibody production
04

Disease associations

Infection (as vaccine adjuvant, including for HBV and COVID-19)Cancer (as immunotherapeutic adjuvant)Allergy (as immunotherapy adjuvant)
05

Safety considerations

Potential induction of excessive inflammationAutoimmunity risk (theoretical; not common at clinical doses)Reactogenicity (injection site and systemic symptoms, similar to other immune adjuvants)
06

Interacting drugs

Adjuvanted vaccines such as HEPLISAV-B (contains CpG 1018)

1 more in the full profile.

07

Biomarkers

Increased antibody titers (e.g., anti-HBs in hepatitis B vaccination)Th1/Th2 cytokine profiles (e.g., IFN-γ, IL-12)Upregulation of activation markers on dendritic cells and B cells (e.g., CD80/86, MHC class II)

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