Prunustatin A, a novel GRP78 molecular chaperone down-regulator isolated from Streptomyces violaceoniger.

Abstract

In the course of our screening program for regulators of a molecular chaperone GRP78 expression, we isolated a novel inhibitor of GRP78 expression, designated as prunustatin A, from Streptomyces violaceoniger 4521-SVS3. The structure of prunustatin A was determined by a series of NMR analyses to be an oxidized type of the neoantimycin family. Prunustatin A inhibited the expression of GRP78 induced by 2-deoxyglucose in human fibrosarcoma HT1080 cells accompanied by global cell death without showing cytotoxicity under normal nutrient condition.

• Authors: Yukiko Umeda, Shuhei Chijiwa, Kazuo Furihata, Keiko Furihata, Shohei Sakuda, Hiromichi Nagasawa, Hidenori Watanabe, Kazuo Shin-ya
• Journal: The Journal of antibiotics (J Antibiot (Tokyo)) Vol. 58 Issue 3 Pg. 206-9 (Mar 2005) ISSN: 0021-8820 [Print] England
• PMID: 15895530 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Endoplasmic Reticulum Chaperone BiP
• HSPA5 protein, human
• Heat-Shock Proteins
• Macrolides
• Molecular Chaperones
• prunustatin A
• Deoxyglucose
• Luciferases

Topics

• Cell Line
• Chemical Phenomena
• Chemistry, Physical
• Deoxyglucose (pharmacology)
• Down-Regulation (drug effects)
• Endoplasmic Reticulum Chaperone BiP
• Genes, Reporter
• Heat-Shock Proteins (antagonists & inhibitors, genetics)
• Humans
• Luciferases (genetics)
• Macrolides (chemistry, isolation & purification, pharmacology)
• Magnetic Resonance Spectroscopy
• Molecular Chaperones (antagonists & inhibitors, genetics)
• Molecular Structure
• Promoter Regions, Genetic
• Spectrometry, Mass, Fast Atom Bombardment
• Streptomyces (chemistry, isolation & purification)