| RRC ID |
44716
|
| 著者 |
Futamura Y, Kawatani M, Muroi M, Aono H, Nogawa T, Osada H.
|
| タイトル |
Identification of a molecular target of a novel fungal metabolite, pyrrolizilactone, by phenotypic profiling systems.
|
| ジャーナル |
Chembiochem
|
| Abstract |
In the course of screening our microbial metabolite fraction library, we identified a novel pyrrolizidinone compound, pyrrolizilactone. In this study, we report the identification and characterization of a molecular target for pyrrolizilactone by using two phenotypic profiling systems. Cell morphology-based profiling analysis using an imaging cytometer (MorphoBase) classified pyrrolizilactone as a proteasome inhibitor. Consistently, proteome-based profiling analysis using 2D difference gel electrophoresis (DIGE; ChemProteoBase) also demonstrated that pyrrolizilactone is associated with proteasome inhibition. On the basis of these predictions, we determined that pyrrolizilactone is a novel type of proteasome inhibitor inhibiting the trypsin-like activity of the proteasome.
|
| 巻・号 |
14(18)
|
| ページ |
2456-63
|
| 公開日 |
2013-12-16
|
| DOI |
10.1002/cbic.201300499
|
| PMID |
24166831
|
| MeSH |
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Biological Products / chemistry
Biological Products / pharmacology*
Databases, Factual
Fungi / chemistry*
HeLa Cells
Humans
Lactones / chemistry
Lactones / pharmacology*
Molecular Targeted Therapy*
Neoplasms / drug therapy
Neoplasms / enzymology
Proteasome Inhibitors / chemistry
Proteasome Inhibitors / pharmacology*
|
| IF |
2.576
|
| 引用数 |
18
|
|
WOS 分野
|
CHEMISTRY, MEDICINAL
BIOCHEMISTRY & MOLECULAR BIOLOGY
|
| リソース情報 |
| ヒト・動物細胞 |
|
