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J Antibiot (Tokyo) ; 50(1): 1-7, 1997 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-9066758

RESUMEN

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.


Asunto(s)
Transferasas Alquil y Aril , Inhibidores Enzimáticos/aislamiento & purificación , Fermentación , Hongos/clasificación , Anhídridos Maleicos/aislamiento & purificación , Transferasas/antagonistas & inhibidores , Animales , Inhibidores Enzimáticos/farmacología , Farnesil Difosfato Farnesil Transferasa/antagonistas & inhibidores , Hongos/metabolismo , Anhídridos Maleicos/farmacología , Ratas
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