Table 1.
Drugs | Targets | Effect on epigenetics or biology |
---|---|---|
Targeting trained immunity | ||
BCG vaccine | Mycobacterium tuberculosis | H3K4 trimethylation of monocytes |
B-glucans | Dectin-1 and complement receptor 3 (CR3) | H3K4 and H3K9 trimethylation |
MDP | NOD2 | Activate NF-κB pathway |
Statins | Mevalonate | Change DNA methylation and prevent trained immunity induction |
B-hydroxybutyrate and MCC950 | NLRP3 | Inhibit NLRP3 inflammasome-mediated trained immunity |
Targeting innate immune signaling | ||
ODNs | TLR9 | Active innate immune responses by producing proinflammation cytokines and Th1 cells |
Imiquimod | TLR7 | Reverse local immunosuppression and induce tumor cell specific apoptosis |
poly(I:C) | TLR9 | Induce stable maturation of functionally active dendritic cells |
TLR3 | Induce cancer cell apoptosis | |
Flagellin-protein fusions | TLR5 | Induces inflammatory responses through the activation of APCs |
IRAK1/4 inhibitor I | IRAK1/4 | Suppresses solid tumor growth in several distinct combination therapies |
NCGC1481 | FLT3-IRAK1/4 | Eliminates adaptive resistance of FLT3-mutant AML cells |
NG25 | TAK1 | Inhibits colorectal cancer cell proliferation, especially for KRAS-mutant cells |
5Z-7-oxozeaenol | TAK1 | Enhances the sensitivity of glioblastoma cells to chemotherapy |
Suppresses triple-negative breast cancer metastasis by altering TAK1-p38 signaling | ||
C-178, C-176 | STING | Inhibits STING palmitoylation and attenuates autoinflammatory features in mice |
NCGC00138783, Pep-20, etc. | CD47/SIRPα | Small-molecule inhibitors targeting macrophage checkpoints that induce phagocytosis |
Abbreviations: MDP, muramyl dipeptide; ODN, CpG oligo-deoxynucleotides.