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Chemical Compound Review

Erbstatin     N-[(E)-2-(2,5- dihydroxyphenyl) ethenyl]meth...

Synonyms: CHEMBL47986, NSC-606641, NSC-610187, LS-69467, NSC606641, ...
 
 
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Disease relevance of Erbstatin

 

High impact information on Erbstatin

 

Biological context of Erbstatin

  • Pre-incubation with erbstatin decreased the amount of tyrosine phosphorylation induced by the formylated oligopeptide formyl-methionyl-leucyl-phenylalanine (fMet-Leu-Phe) without effecting the binding of [3H]-fMet-Leu-Phe [9].
  • Thus, erbstatin-induced apoptosis would be due to hydrogen peroxide generation via newly synthesized protein [10].
  • We also demonstrated that erbstatin-induced hydrogen peroxide production and DNA fragmentation were partially suppressed by inhibition of protein synthesis [10].
  • Genistein, erbstatin, and tyrphostin B42 did not inhibit the early events of fertilization such as elevation of the fertilization envelope; however, later events such as pronuclear migration, DNA synthesis, and cell division were inhibited [11].
  • In the present study, we demonstrated that induction of apoptosis by erbstatin resulted in activation of caspase-3(-like) proteases, which are interleukin-1 beta-converting enzyme family proteases (caspases) and that inhibition of these protease activities reduced the extent of cell death and H2O2 generation [12].
 

Anatomical context of Erbstatin

 

Associations of Erbstatin with other chemical compounds

 

Gene context of Erbstatin

  • The kinetics of inhibition of the epidermal growth factor (EGF) receptor (EGFR) tyrosine kinase (TK) activity by erbstatin, tyrphostins, and lavendustin derivatives were studied in a system that employs poly(Glu6Ala3Tyr) (GAT) and ATP as substrates, after preactivation with EGF [21].
  • Erbstatin inhibited both EGF-induced and serum-stimulated cell growth of all 6 cell lines (TMK-1, MKN-1, -7, -28, -45, -74) in a dose-dependent manner [14].
  • The expression of mRNA of EGF receptor gene and ERBB-2 by TMK-1 cells was not changed by erbstatin treatment, whereas that of c-src was slightly decreased [14].
  • In contrast, activation of MEK-1 was induced by phorbol esters, and the stimulatory effect of fMLP was blocked by an antagonist of protein kinase C. Stimulation of MEK-1 was also blocked by concentrations of erbstatin that prevent the fMLP-induced accumulation of tyrosine-phosphorylated proteins [22].
  • Interestingly, erbstatin decreased membrane-bound TGF-alpha precursor as measured by anti-TGF-alpha antibody-binding assay, although mRNA expression for TGF-alpha was not altered by erbstatin [14].
 

Analytical, diagnostic and therapeutic context of Erbstatin

References

  1. Induction of morphological change by tyrosine kinase inhibitors in Rous sarcoma virus-transformed rat kidney cells. Umezawa, K., Tanaka, K., Hori, T., Abe, S., Sekizawa, R., Imoto, M. FEBS Lett. (1991) [Pubmed]
  2. Antitumor activity of erbstatin, a tyrosine protein kinase inhibitor. Imoto, M., Umezawa, K., Komuro, K., Sawa, T., Takeuchi, T., Umezawa, H. Jpn. J. Cancer Res. (1987) [Pubmed]
  3. Induction of morphological and enzymic differentiation in rat pheochromocytoma PC12h cells by stable erbstatin analogues. Watanabe, Y., Kakeya, H., Ikoma, E., Umezawa, K. Drugs under experimental and clinical research. (1993) [Pubmed]
  4. The anti-proliferative effects of tyrosine kinase inhibitors towards tamoxifen-sensitive and tamoxifen-resistant human breast cancer cell lines in relation to the expression of epidermal growth factor receptors (EGF-R) and the inhibition of EGF-R tyrosine kinase. El-Zarruk, A.A., van den Berg, H.W. Cancer Lett. (1999) [Pubmed]
  5. Tyrosine kinase inhibitors can differentially inhibit integrin-dependent and CAM-stimulated neurite outgrowth. Williams, E.J., Walsh, F.S., Doherty, P. J. Cell Biol. (1994) [Pubmed]
  6. Ca2+-independent activation of the endothelial nitric oxide synthase in response to tyrosine phosphatase inhibitors and fluid shear stress. Fleming, I., Bauersachs, J., Fisslthaler, B., Busse, R. Circ. Res. (1998) [Pubmed]
  7. Regulation of stimulated integrin surface expression in human neutrophils by tyrosine phosphorylation. Naccache, P.H., Jean, N., Liao, N.W., Bator, J.M., McColl, S.R., Kubes, P. Blood (1994) [Pubmed]
  8. Involvement of tyrosine kinases in the activation of human peripheral blood neutrophils by granulocyte-macrophage colony-stimulating factor. McColl, S.R., DiPersio, J.F., Caon, A.C., Ho, P., Naccache, P.H. Blood (1991) [Pubmed]
  9. Selective inhibition of human neutrophil functional responsiveness by erbstatin, an inhibitor of tyrosine protein kinase. Naccache, P.H., Gilbert, C., Caon, A.C., Gaudry, M., Huang, C.K., Bonak, V.A., Umezawa, K., McColl, S.R. Blood (1990) [Pubmed]
  10. Involvement of hydrogen peroxide production in erbstatin-induced apoptosis in human small cell lung carcinoma cells. Simizu, S., Imoto, M., Masuda, N., Takada, M., Umezawa, K. Cancer Res. (1996) [Pubmed]
  11. Effects of protein tyrosine kinase inhibitors on egg activation and fertilization-dependent protein tyrosine kinase activity. Moore, K.L., Kinsey, W.H. Dev. Biol. (1995) [Pubmed]
  12. Induction of hydrogen peroxide production and Bax expression by caspase-3(-like) proteases in tyrosine kinase inhibitor-induced apoptosis in human small cell lung carcinoma cells. Simizu, S., Umezawa, K., Takada, M., Arber, N., Imoto, M. Exp. Cell Res. (1998) [Pubmed]
  13. Tyrosine phosphorylation is involved in reorganization of the actin cytoskeleton in response to serum or LPA stimulation. Chrzanowska-Wodnicka, M., Burridge, K. J. Cell. Sci. (1994) [Pubmed]
  14. Effects of tyrosine kinase inhibitor, erbstatin, on cell growth and growth-factor/receptor gene expression in human gastric carcinoma cells. Takekura, N., Yasui, W., Kyo, E., Yoshida, K., Kameda, T., Kitadai, Y., Abe, K., Umezawa, K., Tahara, E. Int. J. Cancer (1991) [Pubmed]
  15. Insulin stimulation of Na/H antiport in L-6 cells: a different mechanism in myoblasts and myotubes. Incerpi, S., Rizvi, S.I., De Vito, P., Luly, P. J. Cell. Physiol. (1997) [Pubmed]
  16. Thapsigargin-induced calcium influx in the absence of detectable tyrosine phosphorylation in human platelets. Vostal, J.G., Shafer, B. J. Biol. Chem. (1996) [Pubmed]
  17. Chemotactic peptide-induced activation of Ras in human neutrophils is associated with inhibition of p120-GAP activity. Zheng, L., Eckerdal, J., Dimitrijevic, I., Andersson, T. J. Biol. Chem. (1997) [Pubmed]
  18. Modulation of the Kv1.3 potassium channel by receptor tyrosine kinases. Bowlby, M.R., Fadool, D.A., Holmes, T.C., Levitan, I.B. J. Gen. Physiol. (1997) [Pubmed]
  19. Thrombin receptor expression is increased by angiotensin II in cultured and native vascular smooth muscle cells. Fisslthaler, B., Schini-Kerth, V.B., Fleming, I., Busse, R. Cardiovasc. Res. (1998) [Pubmed]
  20. Erbstatin blocks platelet activating factor-induced protein-tyrosine phosphorylation, polyphosphoinositide hydrolysis, protein kinase C activation, serotonin secretion and aggregation of rabbit platelets. Salari, H., Duronio, V., Howard, S.L., Demos, M., Jones, K., Reany, A., Hudson, A.T., Pelech, S.L. FEBS Lett. (1990) [Pubmed]
  21. Kinetics of inhibition by tyrphostins of the tyrosine kinase activity of the epidermal growth factor receptor and analysis by a new computer program. Posner, I., Engel, M., Gazit, A., Levitzki, A. Mol. Pharmacol. (1994) [Pubmed]
  22. Chemotactic peptides induce phosphorylation and activation of MEK-1 in human neutrophils. Grinstein, S., Butler, J.R., Furuya, W., L'Allemain, G., Downey, G.P. J. Biol. Chem. (1994) [Pubmed]
  23. Inhibition of DNA topoisomerases I and II and induction of apoptosis by erbstatin and tyrphostin derivatives. Markovits, J., Larsen, A.K., Ségal-Bendirdjian, E., Fossé, P., Saucier, J.M., Gazit, A., Levitzki, A., Umezawa, K., Jacquemin-Sablon, A. Biochem. Pharmacol. (1994) [Pubmed]
 
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