Difference between revisions of "Selinexor (Xpovio)"
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(Created page with "=Mechanism of action= From [http://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=734824 NCI Drug Dictionary]: An orally available, small molecule inhibitor of CRM...") |
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Revision as of 19:34, 13 July 2017
Mechanism of action
From NCI Drug Dictionary: An orally available, small molecule inhibitor of CRM1 (chromosome region maintenance 1 protein, exportin 1 or XPO1), with potential antineoplastic activity. Selinexor modifies the essential CRM1-cargo binding residue cysteine-528, thereby irreversibly inactivating 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.