title: Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis.
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 IC(50) 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.
authors.affiliation: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, PR China.
authors.forename: Yong-Ming
authors.initials: YM
authors.lastname: Yan
authors.forename: Huan-Qin
authors.initials: HQ
authors.lastname: Dai
authors.forename: Yuhong
authors.initials: Y
authors.lastname: Du
authors.forename: Bernd
authors.initials: B
authors.lastname: Schneider
authors.forename: Hui
authors.initials: H
authors.lastname: Guo
authors.forename: Dian-Peng
authors.initials: DP
authors.lastname: Li
authors.forename: Li-Xin
authors.initials: LX
authors.lastname: Zhang
authors.forename: Haian
authors.initials: H
authors.lastname: Fu
authors.forename: Xiao-Ping
authors.initials: XP
authors.lastname: Dong
authors.forename: Yong-Xian
authors.initials: YX
authors.lastname: Cheng
mesh_terms: D048948:14-3-3 Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D019556:COS Cells; D002522:Chlorocebus aethiops; D002839:Chromans / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D001517:Coleoptera / Q000737:chemistry*; D004797:Enzyme-Linked Immunosorbent Assay; D000431:Ethanol; D009682:Magnetic Resonance Spectroscopy; D010648:Phenylacetates / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D012997:Solvents; D013329:Structure-Activity Relationship; D014020:Tissue Extracts / Q000737:chemistry
chemical_list: D048948:14-3-3 Proteins; D000970:Antineoplastic Agents; D002839:Chromans; D010648:Phenylacetates; D012997:Solvents; D014020:Tissue Extracts; C575105:blapsin A; C575106:blapsin B; D000431:Ethanol