| Autor: |
Dabrah TT; Pfizer Central Research, Groton, CT 06340, USA., Harwood HJ Jr, Huang LH, Jankovich ND, Kaneko T, Li JC, Lindsey S, Moshier PM, Subashi TA, Therrien M, Watts PC |
| Jazyk: |
angličtina |
| Zdroj: |
The Journal of antibiotics [J Antibiot (Tokyo)] 1997 Jan; Vol. 50 (1), pp. 1-7. |
| DOI: |
10.7164/antibiotics.50.1 |
| Abstrakt: |
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 microM and 20 microM, respectively. CP-225,917 inhibits squalene synthase with an IC50 value of 43 microM and CP-263,114 with an IC50 of 160 microM. The producing organism, though not fully classified, exhibits the characteristics of a sterile Phoma species. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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