Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.
Publication
, Journal Article
deSolms, SJ; Ciccarone, TM; MacTough, SC; Shaw, AW; Buser, CA; Ellis-Hutchings, M; Fernandes, C; Hamilton, KA; Huber, HE; Kohl, NE; Lobell, RB ...
Published in: J Med Chem
July 3, 2003
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.
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Published In
J Med Chem
DOI
ISSN
0022-2623
Publication Date
July 3, 2003
Volume
46
Issue
14
Start / End Page
2973 / 2984
Location
United States
Related Subject Headings
- ras Proteins
- rap1 GTP-Binding Proteins
- Tumor Cells, Cultured
- Transplantation, Heterologous
- Structure-Activity Relationship
- Protein Prenylation
- Neoplasms, Experimental
- Neoplasm Transplantation
- Models, Molecular
- Mice, Nude
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deSolms, S. J., Ciccarone, T. M., MacTough, S. C., Shaw, A. W., Buser, C. A., Ellis-Hutchings, M., … Taylor, J. S. (2003). Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents. J Med Chem, 46(14), 2973–2984. https://doi.org/10.1021/jm020587n
deSolms, S Jane, Terrence M. Ciccarone, Suzanne C. MacTough, Anthony W. Shaw, Carolyn A. Buser, Michelle Ellis-Hutchings, Christine Fernandes, et al. “Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.” J Med Chem 46, no. 14 (July 3, 2003): 2973–84. https://doi.org/10.1021/jm020587n.
deSolms SJ, Ciccarone TM, MacTough SC, Shaw AW, Buser CA, Ellis-Hutchings M, et al. Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents. J Med Chem. 2003 Jul 3;46(14):2973–84.
deSolms, S. Jane, et al. “Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.” J Med Chem, vol. 46, no. 14, July 2003, pp. 2973–84. Pubmed, doi:10.1021/jm020587n.
deSolms SJ, Ciccarone TM, MacTough SC, Shaw AW, Buser CA, Ellis-Hutchings M, Fernandes C, Hamilton KA, Huber HE, Kohl NE, Lobell RB, Robinson RG, Tsou NN, Walsh ES, Graham SL, Beese LS, Taylor JS. Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents. J Med Chem. 2003 Jul 3;46(14):2973–2984.
Published In
J Med Chem
DOI
ISSN
0022-2623
Publication Date
July 3, 2003
Volume
46
Issue
14
Start / End Page
2973 / 2984
Location
United States
Related Subject Headings
- ras Proteins
- rap1 GTP-Binding Proteins
- Tumor Cells, Cultured
- Transplantation, Heterologous
- Structure-Activity Relationship
- Protein Prenylation
- Neoplasms, Experimental
- Neoplasm Transplantation
- Models, Molecular
- Mice, Nude