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Cited by 285

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 access
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·Proceedings of the National Academy of Sciences

Abstract

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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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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CoChat. (2026). Citation check: Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice. https://app.cochat.ai/papers/10.1073/pnas.91.19.9141
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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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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

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