Nuclear Export Inhibitors
Nuclear export, mediated mainly by the nuclear export factor exportin-1(Xpo1), also known as chromosomal region maintenance 1 (CRM1), is an essential function in all eukaryote that transport nuclear export signal (NES) containing cargoes from the nucleus to the cytoplasm. Upregulation of this process is a common characteristic for a variety of cancers. CRM1 controls cellular localization and function of numerous proteins that are critical for the development of many cancer hallmarks. Treating cancer through inhibition of nuclear export is one of the best examples of basic research translation into clinical application. Earlier approaches to target CRM1 led to the development of leptomycin B (LMB) which proved to have limited clinical applicability due to its high toxicity and minimal efficacy. Recently, several second generation Selective Inhibitors of Nuclear Export (SINE) have been developed as anticancer drugs that are currently in clinical trials against both solid tumors and hematological malignancies. BioVision is proud to offer a variety of CRM1 inhibitors for research. |
