期刊
DRUG DISCOVERY TODAY
卷 22, 期 12, 页码 1782-1791出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2017.07.013
关键词
-
资金
- NIH, National Institute of Diabetes and Digestive and Kidney Diseases
A single molecular scaffold can be adapted to interact with diverse targets, either separately or simultaneously. Nucleosides and nucleotides in which ribose is substituted with bicyclo[3.1.0]hexane are an example of a versatile drug-like scaffold for increasing selectivity at their classical targets: kinases, polymerases, adenosine and P2 receptors. Also, by applying structure-based functional group manipulations, rigidified adenosine derivatives can be repurposed to satisfy pharmacophoric requirements of various GPCRs, ion channels, enzymes and transporters, initially detected as off-target activities. Recent examples include 5HT(2B) serotonin receptor antagonists and novel dopamine transporter allosteric modulators. This directable target diversity establishes rigid nucleosides as privileged scaffolds.
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