Momoko Akiyama, Ryosuke Ueki, Masataka Yanagawa, Mitsuhiro Abe, Michio Hiroshima, Yasushi Sako, and Shinsuke Sando
Designing synthetic surrogates of functional proteins is an important, albeit challenging, task in the field of chemistry. A strategy toward the design of synthetic agonists for growth factor or cytokine receptors that elicit a desired signal activity has been in high demand, as such ligands hold great promise as safer and more effective therapeutics. In the present study, we used a DNA aptamer as a building block and described the strategy-guided design of a synthetic receptor agonist with fine-tuned agonism. The developed synthetic partial agonist can regulate therapeutically relevant cellular activities by eliciting fine-tuned receptor signaling.
Angewandte Chemie International Edition : https://onlinelibrary.wiley.com/doi/10.1002/anie.202105314