In 2016,Gao, Dong; Zeng, Juan; Wang, Xiaodong; Liu, Yu; Li, Wang; Hu, Yunlong; Gao, Ningning; Diao, Yuwen; Wang, Zhulin; Jiang, Wenqi; Chen, Jinhua; Jin, Guangyi published 《Conjugation of weak ligands with weak antigens to activate TLR-7: A step toward better vaccine adjuvants》.European Journal of Medicinal Chemistry published the findings.Computed Properties of C4H7BrO2 The information in the text is summarized as follows:
To study the structure-activity relationship (SAR) of Toll-like receptor 7 (TLR-7) agonists based on 8-oxoadenines, a novel subset of C9-substituted 8-hydroxy-2-(2-methoxyethoxy)-adenines and their antigen conjugates were synthesized. In vitro, the ability of cytokines (IL-12p70 and IFN-γ) induction of ligands with alkyl acid at C9-position were very weak compared with benzoic acid counter parts. Unexpectedly, its antigen conjugates that conjugated with proteins or peptides with weak immunogenicity, showed enhanced activity of cytokines induction. After administered systemically in mice in vivo, all conjugates induced prolonged increase in pro-inflammatory cytokines and antigen-specific IgG levels in serum compared with free compounds Results from mol. dynamics (MD) simulations further confirmed the conclusion and provided the details of interaction to explain the phenomenon of experiment In conclusion, we discovered that TLR-7 could be activated via some conjugates of weak ligand and weak antigen, which could be safer adjuvant candidates for vaccines in the future. The experimental process involved the reaction of Methyl 3-bromopropanoate(cas: 3395-91-3Computed Properties of C4H7BrO2)
Methyl 3-bromopropanoate(cas: 3395-91-3) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Computed Properties of C4H7BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary