Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 24, Pages 6319-6320Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.10.110
Keywords
Ubc13; E2; Ubiquitin; p53; Anti-cancer
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Funding
- Ministry of Education, Culture, Sports, Science, and Technology of Japan [18032033, 19310140]
- Naito Foundation
- Keimeikai Foundation
- Grants-in-Aid for Scientific Research [19310140, 18032033] Funding Source: KAKEN
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A compound that inhibits the formation of a complex composed of the ubiquitin E2 enzyme Ubc13 and Uev1A was isolated from the marine sponge Leucetta aff. microrhaphis. The compound was identified as leucettamol A (1) by spectroscopic analysis. Its inhibition of Ubc13-Uev1A interaction was tested by the ELISA method, revealing an IC(50) value of 50 mu g/mL. The compound is the first inhibitor of Ubc13-Uev1A interaction, that is, that of the E2 activity of Ubc13. Such inhibitors are presumed to be leads for anti-cancer agents that upregulate activity of the tumor suppressor p53 protein. Interestingly, hydrogenation of 1 increased its inhibitory activity with an IC(50) value of 4 mu g/mL, while its tetraacetate derivative was inactive, indicating that the hydroxy and/or amino groups of 1 are required for the inhibition. (C) 2008 Elsevier Ltd. All rights reserved.
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