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Oct 11, 2011

Karyopharm Teams with Rega Institute to Bolster Nuclear Export Inhibitor Pipeline

  • Karyopharm Therapeutics is teaming up with the Katholieke University of Leuven’s Rega Institute for Medical Research in Belgium to identify selective inhibitors of nuclear export (SINE) modulators of the CRM1 protein. The aim is to expand Karyopharm’s SINE CRM1 antagonist pipeline for the potential treatment of cancer, autoimmune diseases, and viral infections. The firm says the Rega Institute team has pioneered work in the area of nuclear export modulation, particularly in the field of viral replication.

    Founded in 2008, Karyopharm is developing small molecule drugs that modulate the activity of critical pathways in cancer, inflammation, and cell proliferation by targeting the nuclear pore complex machinery that controls the import and export of key regulatory and tumor suppressor proteins between the nucleus and cytoplasm.

    Initial in-house target, Crm1, is the main exporter of key tumor suppressor and growth regulatory proteins such as p53, p21, FOXO, and pRB. The firm says studies have suggested that Crm1 overexpression is linked with with poor prognosis in ovarian, cervical, pancreatic, and liver cancers, as well as osteosarcoma and gliomas. Karyopharm has used its in silico technology platform to identify and optimize small molecule SINE candidates, with a view to progress a lead anticancer candidate into clinical trials in 2012. The firm is in addition evaluating the SINE approach for the treatment of autoimmune, viral, and dermatological disorders. 


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