About: CRM1 Nuclear Export Inhibitor KPT-330

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Attributes	Values
rdf:type	Class
rdfs:label	CRM1 Nuclear Export Inhibitor KPT-330
rdfs:subClassOf	ANTINEOPLASTICS
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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