Bioorganic and Medicinal Chemistry Letters p. 5792 - 5795 (2014)
Update date:2022-08-30
Topics:
Gao, Dong
Liu, Yu
Li, Wang
Zhong, Fangshu
Zhang, Xiaoli
Diao, Yuwen
Gao, Ningning
Wang, Xiaodong
Jiang, Wenqi
Jin, Guangyi
In the synthesis and modification of the analogs of an adenine type of Toll-like receptor (TLR) 7 agonists, we found a special compound, 9-propionyloxy-8-hydroxy-2-(2-methoxyethoxy)-adenine (6). It is a synthesized TLR7 inert ligand, which does not respond to TLR7 itself. However, it can be coupled with protein or peptide antigens via propionyloxy functional group to promote their immunogenicity significantly. The compound was covalently coupled to protein and peptide to get the conjugates. The inductivity of cytokine production by the conjugates was 872.4-fold compared with the unconjugated antigens in vitro by mouse splenocyte. These data show that the immunostimulatory activity of inert TLR7 ligand can be endowed, and the activity of antigens can be amplified by conjugation with various proteins and peptides, thus broadening the potential therapeutic application and reducing the risk of TLR7 agonists' side effects.
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