Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis
Yan, Yong-Ming1,2; Dai, Huan-Qin3; Du, Yuhong4,5; Schneider, Bernd6; Guo, Hui3; Li, Dian-Peng7; Zhang, Li-Xin1,3; Fu, Haian1,4,5; Dong, Xiao-Ping2; Cheng, Yong-Xian1,2
Corresponding AuthorCheng, YX (reprint author), Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China,lzhang03@gmail.com ; hfu@emory.edu ; yxcheng@mail.kib.ac.cn
2012-06-15
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
Volume22Issue:12Pages:4179-4181
AbstractIn 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 mu M as determined by an ELISA assay, and 2.0 and 2.5 mu M in an FP assay, respectively. These compounds represent the first example of natural small-molecule 14-3-3 inhibitors. (C) 2012 Elsevier Ltd. All rights reserved.
KeywordBlaps Japanensis Insects Phenolics 14-3-3 Protein-protein Interactions
Subject AreaPharmacology & Pharmacy ; Chemistry
DOI10.1016/j.bmcl.2012.04.027
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy ; Chemistry
WOS SubjectChemistry, Medicinal ; Chemistry, Organic
WOS IDWOS:000304484600066
Citation statistics
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/17605
Collection植物化学与西部植物资源持续利用国家重点实验室
Affiliation1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China
2.Chengdu Univ Tradit Chinese Med, Coll Pharm, Chengdu 610075, Peoples R China
3.Chinese Acad Sci, Inst Microbiol, Beijing 100101, Peoples R China
4.Emory Univ, Sch Med, Dept Pharmacol, Atlanta, GA 30322 USA
5.Emory Univ, Sch Med, Emory Chem Biol Discovery Ctr, Atlanta, GA 30322 USA
6.Max Planck Inst Chem Ecol, D-07745 Jena, Germany
7.Guangxi Inst Bot, Guangxi Key Lab Funct Phytochem Res & Utilizat, Guilin 541006, Peoples R China
Recommended Citation
GB/T 7714
Yan, Yong-Ming,Dai, Huan-Qin,Du, Yuhong,et al. Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(12):4179-4181.
APA Yan, Yong-Ming.,Dai, Huan-Qin.,Du, Yuhong.,Schneider, Bernd.,Guo, Hui.,...&Cheng, Yong-Xian.(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.
MLA Yan, Yong-Ming,et al."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(2012):4179-4181.
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