中国药理学通报Issue(6)：749-754,6.DOI:10.3969/j.issn.1001-1978.2015.06.003
不可逆性酪氨酸激酶抑制剂的研究进展
Research progress on irreversible tyrosine kinase inhibitors
摘要
Abstract
Dysfunction in tyrosine kinase activity disrupts the nor-mal control of cellular phosphorylation signaling pathways,which plays a vital role in genesis and development of various tumors, and makes tyrosine kinases a class of targets of many anti-tumor drugs. Currently most approved tyrosine kinase inhibitors ( TKIs) are based on irreversible binding mechanisms, making them poorly selective, not potent or sustained enough regarding pharmacological effects and prone to triggering resistance. In the past decade, much progress has been made in the development of <br> a new class of TKIs which irreversibly inhibit their target proteins via the formation of covalent bonds, overcoming the drawbacks of irreversible TKIs. Several irreversible TKIs have entered markets or clinical research phases. This review is to summarize the structural, pharmacological and medicinal chemical properties of investigational and marketed irreversible TKIs as well as their re-cent developments.关键词
酪氨酸激酶/抑制剂/抗肿瘤药物/不可逆/共价结合/ErbB/BTKKey words
tyrosine kinase/inhibitor/anti-tumor drug/irre-versible/covalent binding/ErbB/BTK分类
医药卫生引用本文复制引用
郭建军,朱晶,赵永跃,权腾飞,苗震宇,卜海之..不可逆性酪氨酸激酶抑制剂的研究进展[J].中国药理学通报,2015,(6):749-754,6.基金项目
苏州科学技术局姑苏创新创业领军人才基金的资助( No XG0826) （ No XG0826）
