The DOI matches its Crossref record; 33 of the 33 references it cites were found in a registry or an index.
Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice.
Open accessAbstract
The posttranslational addition of a farnesyl moiety to the Ras oncoprotein is essential for its transforming activity. Cell-active inhibitors of the enzyme that catalyzes this reaction, protein farnesyltransferase, have been shown to selectively block ras-dependent transformation of cells in culture. Here we describe the protein farnesyltransferase inhibitor 2(S)-[2(S)-[2(R)-amino-3-mercapto]propylamino-3(S)-methyl] pentyloxy-3-phenylpropionylmethioninesulfone methyl ester (L-739,749), which suppressed the anchorage-independent growth of Rat1 cells transformed with viral H-ras and the human pancreatic adenocarcinoma cell line PSN-1, which harbors altered K-ras, myc, and p53 genes. This compound also suppressed the growth of tumors arising from ras-transformed Rat1 cells in nude mice by 66%. Under the same conditions, doxorubicin inhibited tumor growth by 33%. Control tumors formed by v-raf- or v-mos-transformed Rat1 cells were unaffected by L-739,749. Furthermore, mice treated with L-739,749 exhibited no evidence of systemic toxicity. This is a demonstration of antitumor activity in vivo using a synthetic small molecule inhibitor of protein farnesyltransferase.
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Cites
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Self-citation
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Differentiation and reversal of malignant changes in colon cancer through PPARγ
Sarraf, P., Mueller, E., Jones, D., King, F. J., DeAngelo, D. J., Partridge, J. B., Holden, S. A., Chen, L. B., Singer, S., Fletcher, C., et al. (1998) · Nature Medicine · doi:10.1038/2030 · Cited by 988
The MYC oncogene — the grand orchestrator of cancer growth and immune evasion
Dhanasekaran, R., Deutzmann, A., Mahauad-Fernandez, W. D., Hansen, A. S., Gouw, A. M., & Felsher, D. W. (2022) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-021-00549-2 · Cited by 986
K- and N-Ras Are Geranylgeranylated in Cells Treated with Farnesyl Protein Transferase Inhibitors
Whyte, D. B., Kirschmeier, P., Hockenberry, T. N., Nunez-Oliva, I., James, L., Catino, J. J., Bishop, W. R., & Pai, J.-K. (1997) · Journal of Biological Chemistry · doi:10.1074/jbc.272.22.14459 · Cited by 884
Targeting protein prenylation for cancer therapy
Berndt, N., Hamilton, A. D., & Sebti, S. M. (2011) · Nature Reviews Cancer · doi:10.1038/nrc3151 · Cited by 614
“However, FTIs are effective at inhibiting the growth of mutant KRAS-harbouring tumours in nude mic”
Ras Protein Farnesyltransferase: A Strategic Target for Anticancer Therapeutic Development
Rowinsky, E. K., Windle, J. J., & Von Hoff, D. D. (1999) · Journal of Clinical Oncology · doi:10.1200/jco.1999.17.11.3631 · Cited by 537
Metadata
- Authors
- Kohl, N. E., Wilson, F. R., Mosser, S. D., Giuliani, E., deSolms, S. J., Conner, M. W., Anthony, N. J., Holtz, W. J., Gomez, R. P., & Lee, T. J.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1994-09-13
- Volume
- 91
- Issue
- 19
- Pages
- 9141-9145
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2107666634
- Cited by
- 285
- References
- 33
- FWCI
- 8.58
- Type
- journal article
- Language
- en
- Open access
- green
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- Kohl, N. E., Wilson, F. R., Mosser, S. D., Giuliani, E., deSolms, S. J., Conner, M. W., Anthony, N. J., Holtz, W. J., Gomez, R. P., & Lee, T. J. (1994). Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.91.19.9141
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