Clavaric Acid: A Triterpenoid Inhibitor of Farnesyl-Protein Transferase from Clavariadelphus truncatus
- 9 October 1998
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Natural Products
- Vol. 61 (12) , 1568-1570
- https://doi.org/10.1021/np980200c
Abstract
Farnesyl-protein transferase (FPTase) catalyses the specific transfer of farnesyl to Ras-peptides that is essential for oncogenic activity in oncogene-mediated tumors. Specific inhibition of FPTase activity has been shown to reduce tumor development in nude mice challenged with oncogenic forms of ras, thereby establishing FPTase as a viable therapeutic target. Our continued efforts to discover inhibitors of FPTase has led to the discovery of a triterpenoidal inhibitor, clavaric acid (1). This compound inhibits rHFPTase with an IC50 value of 1.3 μM. Structure elucidation, structure modifications, and biological activity of clavaric acid are herein described.Keywords
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