Levitzki A
Department of Biological Chemistry, Alexander Silberman Institute of Life Sciences, Hebrew University of Jerusalem, Israel.
FASEB J. 1992 Nov;6(14):3275-82. doi: 10.1096/fasebj.6.14.1426765.
Protein tyrosine kinases (PTKs) are members of a growing family of oncoproteins and protooncoproteins that play a pivotal role in normal and abnormal proliferative processes. This hallmark identifies these unique proteins as potential targets for antiproliferative therapy. This review discusses the current status of PTK inhibitors, with special emphasis on tyrphostins as antiproliferative agents and as potential drugs for cancers, leukemias, psoriasis, and restenosis as well as other proliferative conditions. The development of tyrphostins as selective signal blockers can be viewed as a first step toward the development of "smart" cocktails as antiproliferative agents. Each of these custom-made cocktails will be aimed at proliferative conditions whose transduction pathways can be characterized by molecular tools. The review also discusses the use of PTK blockers as tools to study signal transduction processes in which protein tyrosine kinases are implicated.
蛋白质酪氨酸激酶（PTKs）是一个不断壮大的癌蛋白和原癌蛋白家族的成员，它们在正常和异常增殖过程中起关键作用。这一特性使这些独特的蛋白质成为抗增殖治疗的潜在靶点。本综述讨论了PTK抑制剂的现状，特别强调了 tyrphostins 作为抗增殖剂以及作为癌症、白血病、银屑病和再狭窄以及其他增殖性疾病的潜在药物。tyrphostins 作为选择性信号阻断剂的开发可被视为朝着开发“智能”鸡尾酒抗增殖剂迈出的第一步。这些定制的鸡尾酒中的每一种都将针对其转导途径可用分子工具表征的增殖性疾病。该综述还讨论了PTK阻断剂作为研究涉及蛋白质酪氨酸激酶的信号转导过程的工具的用途。
