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  Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis

Yan, Y.-M., Dai, H.-Q., Du, Y., Schneider, B., Guo, H., Li, D.-P., et al. (2012). Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis. Bioorganic & Medicinal Chemistry Letters, 22(12), 4179-4181. doi:10.1016/j.bmcl.2012.04.027.

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Item Permalink: https://hdl.handle.net/11858/00-001M-0000-000F-A1FC-6 Version Permalink: https://hdl.handle.net/21.11116/0000-0009-337D-2
Genre: Journal Article

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NMR186.pdf (Publisher version), 292KB
 
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Yan, Yong-Ming, Author
Dai, Huan-Qin, Author
Du, Yuhong, Author
Schneider, Bernd1, Author           
Guo, Hui, Author
Li, Dian-Peng, Author
Zhang, Li-Xin, Author
Fu, Haian, Author
Dong, Xiao-Ping, Author
Cheng, Yong-Xian, Author
Affiliations:
1Research Group Biosynthesis / NMR, MPI for Chemical Ecology, Max Planck Society, ou_421898              

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 Abstract: In this study, we report three novel naturally occurring compounds, blapsins A (1) and B (2), and blapsamide (3) from the ethanol extract of the stink beetle, Blaps japanensis. The structures of these compounds were determined using spectroscopic methods. Compound 3 is a phenolic compound bearing a formamido group in the structure. Functional studies revealed that compounds 1 and 2 potently inhibited 14-3-3 protein–protein interactions (PPIs) with IC50 values of 9.2 and 10.0 μM as determined by an ELISA assay, and 2.0 and 2.5 μM in an FP assay, respectively. These compounds represent the first example of natural small-molecule 14-3-3 inhibitors.

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 Dates: 2012-04-122012-06-15
 Publication Status: Issued
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 Identifiers: Other: NMR186
DOI: 10.1016/j.bmcl.2012.04.027
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Title: Bioorganic & Medicinal Chemistry Letters
  Other : Bioorg. Med. Chem. Lett.
Source Genre: Journal
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Publ. Info: Oxford : Pergamon
Pages: - Volume / Issue: 22 (12) Sequence Number: - Start / End Page: 4179 - 4181 Identifier: ISSN: 0960-894X
CoNE: https://pure.mpg.de/cone/journals/resource/954925579103