About: CRM1 Nuclear Export Inhibitor KPT-330     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • CRM1 Nuclear Export Inhibitor KPT-330
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • CRM1 Nuclear Export Inhibitor KPT-330
NCI_META_CUI
  • CL436815
PDQ_Open_Trial_Search_ID
  • 734824
PDQ_Closed_Trial_Search_ID
  • 734824
FULL_SYN
  • SINE KPT-330SYNCI
  • Selective Inhibitor of Nuclear Export KPT-330SYNCI
  • CRM1 Nuclear Export Inhibitor KPT-330PTNCI
  • KPT-330CNNCI
DEFINITION
  • An orally available, small molecule inhibitor of CRM1 (chromosome region maintenance 1 protein, exportin 1 or XPO1), with potential antineoplastic activity. CRM1 nuclear export inhibitor KPT-330 modifies the essential CRM1-cargo binding residue cysteine-528, thereby irreversibly inactivates CRM1-mediated nuclear export of cargo proteins such as tumor suppressor proteins (TSPs), including p53, p21, BRCA1/2, pRB, FOXO, and other growth regulatory proteins. As a result, this agent, via the approach of selective inhibition of nuclear export (SINE), restores endogenous tumor suppressing processes to selectively eliminate tumor cells while sparing normal cells. CRM1, the major export factor for proteins from the nucleus to the cytoplasm, is overexpressed in a variety of cancer cell types.NCI
code
  • C102546
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