CP-225,917 and CP-263,114, Novel Ras Farnesylation Inhibitors from an Unidentified Fungus. I. Taxonomy, Fermentation, Isolation, and Biochemical Properties.
- 1 January 1997
- journal article
- research article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 50 (1) , 1-7
- https://doi.org/10.7164/antibiotics.50.1
Abstract
During the course of our screening for squalene synthase inhibitors and Ras farnesylation inhibitors, a novel fungal culture was discovered to produce two structurally unique compounds, CP-225,917 and CP-263,114, as well as zaragozic acid A (squalestatin I). The two compounds are characterized by a bicyclo[4.3.1]dec-1,6-diene core plus two extended alkyl chains. CP-225,917 and CP-263,114 inhibit Ras farnesyl transferase from rat brain with IC50 values of 6 mu M and 20 mu M, respectively. CP-225,917 inhibits squalene synthase with an IC50 value of 43 mu M and CP-263,114 with an IC50 of 160 mu M. The producing organism, though not fully classified, exhibits the characteristics of a sterile Phoma species.Keywords
This publication has 0 references indexed in Scilit: