Blocking of EGF-Dependent Cell Proliferation by EGF Receptor Kinase Inhibitors

DOI Web Site 被引用文献8件
  • Pnina Yaish
    Department of Biological Chemistry, Hebrew University of Jerusalem, Jerusalem 91 904, Israel.
  • Aviv Gazit
    Department of Organic Chemistry, Hebrew University of Jerusalem, Jerusalem 91 904, Israel.
  • Chaim Gilon
    Department of Organic Chemistry, Hebrew University of Jerusalem, Jerusalem 91 904, Israel.
  • Alexander Levitzki
    Department of Biological Chemistry, Hebrew University of Jerusalem, Jerusalem 91 904, Israel.

抄録

<jats:p>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.</jats:p>

収録刊行物

  • Science

    Science 242 (4880), 933-935, 1988-11-11

    American Association for the Advancement of Science (AAAS)

被引用文献 (8)*注記

もっと見る

キーワード

詳細情報 詳細情報について

問題の指摘

ページトップへ