Science 1988-11-11

Blocking of EGF-dependent cell proliferation by EGF receptor kinase inhibitors.

P Yaish, A Gazit, C Gilon, A Levitzki

文献索引：Science 242(4880) , 933-5, (1988)

全文：HTML全文

摘要

A systematic series of low molecular weight protein tyrosine kinase inhibitors were synthesized; they had progressively increasing affinity over a 2500-fold range toward the substrate site of epidermal growth factor (EGF) receptor kinase domain. These compounds inhibited EGF receptor kinase activity up to three orders of magnitude more than they inhibited insulin receptor kinase, and they also effectively inhibited the EGF-dependent autophosphorylation of the receptor. The most potent compounds effectively inhibited the EGF-dependent proliferation of A431/clone 15 cells with little or no effect on the EGF-independent proliferation of these cells. The potential use of tyrosine protein kinase inhibitors as antiproliferative agents is demonstrated.

相关化合物

  • (3,4-二羟基苄基)丙...
  • 2-氨基-1,1,3-三氰...
  • 酪氨酸磷酸化抑制剂...

相关文献：

Regulation of store-operated Ca2+ entry in pulmonary artery smooth muscle cells.

2009-08-01

[Cell Calcium 46(2) , 99-106, (2009)]

Spatio-temporal cellular dynamics of the Arabidopsis flagellin receptor reveal activation status-dependent endosomal sorting.

2012-10-01

[Plant Cell 24(10) , 4205-19, (2012)]

Swelling-activated K+ efflux and regulatory volume decrease efficiency in human bronchial epithelial cells.

2006-01-01

[J. Membr. Biol. 214(1) , 33-41, (2006)]

Rapid regulation of dopamine transporters by tyrosine kinases in rat neuronal preparations.

2007-06-01

[J. Neurochem. 101(5) , 1258-71, (2007)]

Role of kinases and G-proteins in the hyposmotic stimulation of cardiac IKs.

2006-10-01

[Biochim. Biophys. Acta 1758(10) , 1641-52, (2006)]

更多文献...