Toll-like receptors (TLRs) are interesting targets for immunotherapies and their agonists are currently being explored for anti-viral activity, cancer immunotherapies, and vaccine adjuvants. One particular challenge is making TLR agonists more specific, so that they do not contribute to general activation. Targeted covalent inhibitors have been shown to have irreversible binding with the receptors of interest, leading to high selectivity and potency. These properties are very attractive for TLR agonists. In addition, it is currently not known what effect continuous activation of TLRs will have on immune activation. By applying the design principles of covalent inhibitors to agonists of TLR, we have developed several potential covalent agonists of TLR7 and evaluated them in biological assays.

Progress towards a novel class of immune modulators: Covalent toll-like receptor-7 agonists

253rd National Meeting (2017)

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