Non-peptidic, non-prenylic bisubstrate farnesyltransferase inhibitors, 4. Effect on farnesyltransferase inhibitory activity of conformational restrictions in the central group

Pharmacy and Pharmacology Communications

Volumn 6, Issue 3, 2000, Pages 117-124

  Schlitzer, Martin ^a   Sattler, Isabel ^b  

^a PHILIPPS UNIVERSITY MARBURG   (Germany)

^b HANS KNÖLL INSTITUTE   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

AMINO ACID; PROTEIN FARNESYLTRANSFERASE INHIBITOR;

ARTICLE; CHEMICAL MODIFICATION; DRUG CONFORMATION; DRUG STRUCTURE; ENZYME INHIBITION; STEREOCHEMISTRY;

EID: 0034069058     PISSN: 14608081     EISSN: None     Source Type: Journal    
DOI: 10.1211/146080800128735746     Document Type: Article

References (14)

1. Ciccarone, T. M., MacTough, S. C., Williams, T. M., Dingsmore, C. J., O'Neill, T. J., Shah, D., Culberson, J. C., Koblan, K. S., Kohl, N. E., Gibbs, J. B., Oliff, A. I., Graham, S. L., Hartman, G. D. (1999) Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase. Bioorg. Med. Chem. Lett. 9: 1991-1996
2. Cox, A. D., Der, C. J. (1997) Farnesyltransferase inhibitors and cancer treatment: targeting simply Ras? Biochim. Biophys. Acta 1333: F51-F71
3. Del Villar, K., Mitsuzawa, H., Yang, W., Sattler, I., Tamanoi, F. (1997) Amino acid substitutions that convert the protein substrate specificity of farneslytransferase to that of geranylgeranyltransferase type I. J. Biol. Chem. 272: 680-687
4. Du, W., Lebowitz, P. F., Prendergast, G. C. (1999) Cell growth inhibition by farnesyltransferase inhibitors is mediated by gain of geranylgeranylated RhoB. Mol. Cell. Biol. 19: 1831-1840
5. Gomez, J., Martinez, A. C., Gonzalez, A., Rebollo, A. (1998) Dual role of Ras and Rho proteins: at the cutting edge of life and death. Immunol. Cell Biol. 76: 125-134
6. Leonard, D. M. (1997) Ras farnesyltransferase: a new therapeutic target. J. Med. Chem. 40: 2971-2990
7. Macara, I. G., Lounsbury, K. M., Richards, S. A., McKiernan, C., Bar-Sari, D. (1996) The Ras superfamily of GTPases. FASEB J. 10: 625-630
8. McCormick, K. G. (1999) Signalling networks that cause cancer. Trends Biochem. Sci. 24: M53-M56
9. Pompliano, D. L., Gomez, R. P., Anthony, N. J. (1992) Intramolecular fluorescence enhancement: a continuous assay of Ras farnesyl:protein transferase. J. Am. Chem. Soc. 114: 7945-7946
10. Qian, Y., Sebti, S. M., Hamilton, A. D. (1997) Farnesyltransferase as a target for anticancer drug design. Biopolymers: 43: 25-41
11. Schlitzer, M., Sattler, I. (1999a) Design, synthesis and evaluation of novel modular bisubstrate analogue inhibitors of farnesyltransferase. Angew. Chem. Int. Engl. Ed. 38: 2032-2034
12. Schlitzer, M., Sattler, I., Dahse, H.-M. (1999) Different amino acid replacements in CAAX-tetrapeptide-based farnesyltransferase inhibitors. Arch. Pharm. Pharm. Med. Chem. 332: 124-132
13. Sebti, S. M., Hamilton, A. D. (1998) New approaches to anticancer drug design based on the inhibition of farnesyltransferase. Drug Discov. Today 3: 26-32
14. Zhang, F. L., Casey, P. J. (1996) Protein prenylation: molecular mechanism and functional consequences. Annu. Rev. Biochem 65: 241-269