期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 60, 期 42, 页码 22745-22752出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202105314
关键词
aptamers; growth factors; receptors; signal transduction
资金
- Uehara Memorial Foundation
- AMED [JP20ak0101139]
- Japan Society for the Promotion of Science (JSPS) [19K15693]
- Japan Science and Technology Agency (JST) [JPMJTR20UL]
- Noguchi-Shitagau Research Grant from The Noguchi Institute
- Grants-in-Aid for Scientific Research [19K15693] Funding Source: KAKEN
In this study, a synthetic receptor agonist was designed using a DNA aptamer as a building block to fine-tune agonism. The developed synthetic partial agonist can regulate therapeutically relevant cellular activities by eliciting finely-tuned receptor signaling.
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.
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