| Autor: |
deSolms, S. J., Ciccarone, T. M., MacTough, S. C., Shaw, A. W., Buser, C. A., Ellis-Hutchings, M., Fernandes, C., Hamilton, K. A., Huber, H. E., Kohl, N. E., Lobell, R. B., Robinson, R. G., Tsou, N. N., Walsh, E. S., Graham, S. L., Beese, L. S., Taylor, J. S. |
| Zdroj: |
Journal of Medicinal Chemistry; July 2003, Vol. 46 Issue: 14 p2973-2984, 12p |
| Abstrakt: |
A series of novel diaryl ether lactams have been identified as very potent dual inhibitors of protein farnesyltransferase (FTase) and protein geranylgeranyltransferase I (GGTase-I), enzymes involved in the prenylation of Ras. The structure of the complex formed between one of these compounds and FTase has been determined by X-ray crystallography. These compounds are the first reported to inhibit the prenylation of the important oncogene Ki-Ras4B in vivo. Unfortunately, doses sufficient to achieve this endpoint were rapidly lethal. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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