Ji Ting-Ting, Chen Qiu-Ni, Tao Shan-Dong, Yu Liang
Department of Hematology,Huai'an First People's Hospital Affiliaed to Nanjing Medical University,Huai'an 223300, Jiangsu Province,China,Key Laboratory of Hematology of Nanjing Medical University, Nanjing 210009, Jiangsu Province, China.
Department of Hematology,Huai'an First People's Hospital Affiliaed to Nanjing Medical University,Huai'an 223300, Jiangsu Province,China,Key Laboratory of Hematology of Nanjing Medical University, Nanjing 210009, Jiangsu Province, China,E-mail:
Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2020 Jun;28(3):1054-1058. doi: 10.19746/j.cnki.issn.1009-2137.2020.03.056.
Abstract Spleen tyrosine kinase (SYK) is not only a key kinase in the B-cell receptor (BCR) signaling pathway, but also a critical component of other signal transduction pathways such as Fc receptor, complement receptor and integrin. Abnormal activation of SYK closely related to the occurrence and development of hematological malignancies, thus targeting SYK has become a research hotspot. Several SYK inhibitors including Fostamatinib, Entospletinib and Cerdulatinib were being evaluated in clincal trials. As a second generation SYK inhibitor, Entospletinib has achieved good efficacy in lymphoid and myeloid hematologic tumors. Furthermore, Entospletinib can significantly relieve hematopoietic stem cell transplantation(HCT) related graft versus host disease (GVHD). In this review the role of SYK inhibitors in treatment of hematological malignancies is summarized brifely.
摘要 脾酪氨酸激酶(SYK)不仅是B细胞受体(BCR)信号通路中的关键激酶,也是其他信号转导通路(如Fc受体、补体受体和整合素)的重要组成部分。SYK的异常激活与血液系统恶性肿瘤的发生发展密切相关,因此靶向SYK已成为研究热点。包括福他替尼、恩托司替尼和塞杜替尼在内的几种SYK抑制剂正在进行临床试验评估。作为第二代SYK抑制剂,恩托司替尼在淋巴和髓系血液肿瘤中取得了良好疗效。此外,恩托司替尼可显著缓解造血干细胞移植(HCT)相关的移植物抗宿主病(GVHD)。本文简要综述SYK抑制剂在血液系统恶性肿瘤治疗中的作用。