Selective inhibitors of nuclear export (SINE) in hematological malignancies

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• 作者：Arundhati Das (1)
  Guoqing Wei (2)
  Kaushal Parikh (1)
  Delong Liu (3)
  
  1. Department of Medicine ; Westchester Medical Center ; Valhalla ; NY ; 10595 ; USA
  2. Bone Marrow Transplantation Center ; The First Affiliated Hospital ; Zhejiang University School of Medicine ; Hangzhou ; China
  3. Henan Cancer Hospital ; Zhengzhou University ; Zhengzhou ; China
  
• 关键词：Selective inhibitor of nuclear export ; SINE ; Slinexor ; KPT ; 330
• 刊名：Experimental Hematology & Oncology
• 出版年：2015
• 出版时间：December 2015
• 年：2015
• 卷：4
• 期：1
• 全文大小：415 KB
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• 刊物主题：Hematology; Oncology;
• 出版者：BioMed Central
• ISSN：2162-3619

文摘

Regulated nucleo-cytoplasmic transport plays a major role in maintaining cellular homeostasis. CRM1 (chromosome region maintenance 1 or exportin 1 or XPO 1) is responsible for the nucleo-cytoplasmic transport of more than 200 proteins, including most of the tumor suppressor proteins (TSP). CRM1 is overexpressed in pancreatic cancer, osteosarcoma, glioma, cervical and hematological malignancies. This inspired the development of novel agents that selectively inhibit nuclear exportins (SINEs). In this review we focus on the significance of CRM1 in carcinogenesis and review the new development of SINE inhibitiors in hematological malignancies. Selinexor (KPT-330) as the first-in-human SINE agent represents this novel class of anti-cancer agents.