SAHA and PJ 1548,a Novel Tyrosine Kinase Inhibitor Synergistically Induce Apoptosis in Imatinib-Resi

• 作 者: QianguiBu[1]KeDing[2]JingxuanPan[1]
• 机 构: Department of Pathophysiology,Zhongshan School of Medicine,Sun Yat-sen University,Guangzhou,China
• 出 处: 2012医学科学前沿暨第二届个体化治疗与抗肿瘤药物研究新趋向研讨会
• 发表日期: 2012年期

　　Limited treatment options are available for chronic myeloid leukemia (CML) patients who develop imatinib mesylate resistance particularly in patients with gatekeep mutant Bcr-Abl such as T3151.Compound PJ 1548 was originally designed and synthesized against T3151 Bcr-Abl in our lab.The kinase assay showed that it blocked multiple tyrosine kinases including both wild-type as well as T3151 Bcr-Abl.Despite so,the lesson taken in the clinical application of imatinib and the second-generation of small molecule inhibitors (nilotinib and dasatinib) hint that resistance may arise.