Himeic acid A: a new ubiquitin-activating enzyme inhibitor isolated from a marine-derived fungus, Aspergillus sp

• Published in: Bioorganic & medicinal chemistry letters 2005-01, Vol.15 (1), p.191-194
• Main Authors: Tsukamoto, Sachiko, Hirota, Hiroshi, Imachi, Misako, Fujimuro, Masahiro, Onuki, Hiroyuki, Ohta, Tomihisa, Yokosawa, Hideyoshi
• Format: Article
• Language: English
• Subjects: Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents; Applied microbiology; Aspergillus - chemistry; Aspergillus sp; Biological and medical sciences; Chemotherapic agents; Enzyme Inhibitors - isolation & purification; Enzyme Inhibitors - pharmacology; Fatty Acids, Unsaturated - isolation & purification; Fatty Acids, Unsaturated - pharmacology; Fundamental and applied biological sciences. Psychology; Marine Biology; Marine-derived fungus; Microbiology; Pyrones - isolation & purification; Pyrones - pharmacology; Spectrometry, Mass, Fast Atom Bombardment; Ubiquitin-activating enzyme inhibitor; Ubiquitin-Activating Enzymes - antagonists & inhibitors
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2004.10.012

[Display omitted] A new ubiquitin-activating enzyme (E1) inhibitor, himeic acid A, was isolated from a culture of marine-derived fungus, Aspergillus sp. The structure was determined by spectroscopic analysis. The formation of an E1–ubiquitin (Ub) intermediate was 65% inhibited by himeic acid A at the concentration of 50 μM, while two new related compounds, himeic acids B and C, showed little inhibitory activity even at 100 μM.