Inhibitors of RAS signal transduction as antitumor agents

Biochemical Pharmacology

Volumn 60, Issue 8, 2000, Pages 1165-1169

  Garbay, Christiane ^a   Liu, Wang Qing ^a   Vidal, Michel ^a   Roques, Bernard P ^a  

^a CNRS   (France)

Author keywords

Antitumor agents; Grb2; Ras signaling; SH2; SH3 domain inhibitors

Indexed keywords

ADAPTOR PROTEIN; EPIDERMAL GROWTH FACTOR RECEPTOR; GUANOSINE DIPHOSPHATE; GUANOSINE TRIPHOSPHATE; MITOGEN ACTIVATED PROTEIN KINASE; RAF PROTEIN; RAS PROTEIN; TRANSCRIPTION FACTOR;

ANIMAL CELL; BREAST CANCER; DRUG TARGETING; ENZYME ACTIVITY; LEUKEMIA CELL; NONHUMAN; OVARY CANCER; PRIORITY JOURNAL; REVIEW; SIGNAL TRANSDUCTION; TUMOR CELL;

EID: 0034668178     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(00)00428-7     Document Type: Article

References (24)

1. Lowenstein E.J., Daly R.J., Batzer A.G., Li W., Margolis B., Lammers R., Ullrich A., Skolnik E.Y., Bar-Sagi D., Schlessinger J. The SH2 and SH3 domain-containing protein Grb2 links receptor tyrosine kinases to ras signaling. Cell. 70:1992;431-442.
2. Chardin P., Cussac D., Maignan S., Ducruix A. The Grb2 adaptor. FEBS Lett. 369:1995;47-51.
3. Seger R., Krebs E.G. The MAPK signaling cascade. FASEB J. 9:1995;726-735.
4. Cheng A.L., Saxton T.M., Sakai R., Kulkarni S., Mbamalu G., Vogel W., Tortorice C.G., Cardiff R.D., Cross J.C., Muller W.J., Pawson T. Mammalian Grb2 regulates multiple steps in embryonic development and malignant transformation. Cell. 95:1998;783-803.
5. Jane P.W., Daly R.J., deFazio A., Sutherland R.L. Activation of the Ras signalling pathway in human breast cancer cells overexpressing erbB-2. Oncogene. 9:1994;3601-3608.
6. Pendergast A.M., Quilliam L.A., Cripe L.D., Bassing C.H., Dai Z., Li N., Batzer A., Rabun K.M., Der C.J., Schlessinger J., Gishizky M.L. BCR-ABL-induced oncogenesis is mediated by direct interaction with the SH2 domain of the GRB-2 adaptor protein. Cell. 75:1993;175-185.
7. Xie Y., Pendergast A.M., Huang M.C. Dominant-negative mutants of Grb2 induced reversal of the transformed phenotypes caused by the point mutation-activated rat HER-2/neu. J Biol Chem. 270:1995;30717-30724.
8. Goudreau N., Cornille F., Duchesne M., Parker F., Tocque B., Garbay C., Roques B.P. NMR structure of the N-terminal SH3 domain of Grb2 and its complex with a proline-rich peptide from Sos. Nat Struct Biol. 1:1994;898-907.
9. Kohda D., Terasawa H., Ichikawa S., Ogura K., Hatanaka H., Mandiyan V., Ullrich A., Schlessinger J., Inagaki F. Solution structure and ligand-binding site of the carboxy-terminal SH3 domain of Grb2. Structure. 2:1994;1029-1040.
10. Maignan S., Guilloteau J.P., Fromage N., Arnoux B., Becquart J., Ducruix A. Crystal structure of the mammalian Grb2 adaptor. Science. 268:1995;291-293.
11. Gaugain B., Markovits J., Le Pecq J.B., Roques B.P. DNA polyintercalation Comparison of DNA binding properties of an acridine dimer and trimer . FEBS Lett. 169:1984;123-126.
12. Cussac D., Vidal M., Leprince C., Liu W.Q., Cornille F., Tiraboschi G., Roques B.P., Garbay C. A Sos-derived peptidimer blocks the Ras signaling pathway by binding both Grb2 SH3 domains and displays antiproliferative activity. FASEB J. 13:1999;31-38.
13. Nguyen J.T., Turck C.W., Cohen F.E., Zuckermann R.N., Lim W.A. Exploiting the basis of proline recognition by SH3 and WW domains Design of N-substituted inhibitors . Science. 282:1998;2088-2092.
14. Derossi D., Calvet S., Trembleau A., Brunissen A., Chassaing G., Prochiantz A. Cell internalization of the third helix of the Antennapedia homeodomain is receptor-independent. J Biol Chem. 271:1996;18188-18193.
15. Lin Y.Z., Yao S.Y., Veach R.A., Torgerson T.R., Hawiger J. Inhibition of nuclear translocation of transcription factor NF-κB by a synthetic peptide containing a cell membrane-permeable motif and nuclear localization sequence. J Biol Chem. 270:1995;14255-14258.
16. Vivès E., Brodin P., Lebleu B. A truncated HIV-1 Tat protein basic domain rapidly translocates through the plasma membrane and accumulates in the cell nucleus. J Biol Chem. 272:1997;16010-16017.
17. Rahuel J., Gay B., Erdmann D., Strauss A., Garcia-Echeverria C., Furet P., Caravatti G., Fretz H., Schoepfer J., Grütter M.G. Structural basis for specificity of GRB2-SH2 revealed by a novel ligand binding mode. Nat Struct Biol. 3:1996;586-589.
18. Furet P., Gay B., Garcia-Echeverria C., Rahuel J., Fretz H., Schoepfer J., Caravatti G. Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domain. J Med Chem. 40:1997;3551-3556.
19. Liu W.Q., Vidal M., Gresh N., Roques B.P., Garbay C. Small peptides containing phosphotyrosine and adjacent αMe-phosphotyrosine or its mimetics as highly potent inhibitors of Grb2 SH2 domain. J Med Chem. 42:1999;3737-3741.
20. 2 . J Med Chem. 41:1998;1741-1744.
21. Sawyer T.K. Src homology-2 domains Structure, mechanisms, and drug discovery . Biopolymers. 47:1998;243-261.
22. Garbay C, Liu WQ, Vidal M and Roques BP, Composés pseudopeptidiques dotés d'une activité inhibitrice à l'égard des voies activées par les protéines à activité tyrosine kinase et les compositions pharmaceutiques les contenant. Brevet INSERMFr 98.16459 (24/12/1998).
23. Lefebvre P. I, érigaud C., Pompon A., Aubertin A.M., Girardet J.L., Kirn A., Gosselin G., Imbach J.L. Mononucleoside phosphotriester derivates with S-acyl-2-thioethyl bioreversible phosphate-protecting groups Intracellular delivery of 3′-azido-2′,3′-dideoxythymidine 5′-monophosphate . J Med Chem. 38:1995;3941-3950.
24. Liu W.Q., Vidal M., Mathé C., Périgaud C., Garbay C. Inhibition of the Ras-dependent mitogenic pathway by phosphopeptide prodrugs with antiproliferative properties. Bioorg Med Chem Lett. 10:2000;669-672.