期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 13, 期 2, 页码 304-311出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.1c00671
关键词
Firefly luciferase; small molecule inhibitor; tetralone; bioluminescence
资金
- National Natural Science Foundation of China [81973174, 81803054, 82073869]
Highly potent and reversible Firefly luciferase inhibitors were identified, which have significant applications in constructing novel assay platforms and efficiently blocking the bioluminescence generated by Fluc in vivo.
The extensive applications of Firefly luciferase (Fluc) in numerous biological, biomedical, and clinical investigations rendered an urgent need for efficient and biocompatible Fluc inhibitors for the construction of novel assay platforms. Herein we describe the identification of 2-benzylidene-tetralone derivatives as highly potent and reversible Firefly luciferase inhibitors by competing with D-luciferin. The most active compound 48 was found to have >7000 fold higher potency (IC50 = 0.25 nM) than that of the well-known luciferase inhibitor resveratrol (IC50 = 1.9 mu M) biochemically with sub-to low nanomolar IC50 values, and it can efficiently block the Fluc generated bioluminescence in vivo.
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