生物活性 | |||
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描述 | Toll-like receptors (TLRs) are pattern recognition receptors that play an essential role in host defense against pathogens. TLRs recognize specific pathogen-associated molecular patterns (PAMPs) conserved in viruses, bacteria and other microbes[1]. TLR7 agonist T7 (1V209), a small molecule agonist of Toll-Like receptor 7 (TLR7), is chosen as a proof-of-concept immunotherapeutic. It can be conjugated with various polysaccharides to improve its efficacy, and maintain low toxicity. Intralesional administration of 1V209 reduced the growth of melanoma nodules as well as enhanced the antimelanoma effect of systemic IL-2 treatment. In mice bearing 4T1 tumors, significantly increased levels of all three cytokines (IP-10, MCP-1, and IL-6) were observed in animals administered 1V209. Furthermore, analysis of lung metastases 28 d post-treatments demonstrated that 1V209-L-NP significantly reduced metastases counts relative to saline control. Ex vivo imaging of tumors indicated that 1V209-L-NPF accumulated in the tumor and could be imaged with animal body weights remaining constant and comparable to saline-treated animals. In addition, 1V209-L-NPF is capable of reducing the production of lung metastases[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.78mL 0.56mL 0.28mL |
13.91mL 2.78mL 1.39mL |
27.83mL 5.57mL 2.78mL |
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