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NEW PYRIDOCARBAZOLE COMPOUNDS AND THEIR USES FOR CANCER THERAPY |
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Principal Investigator: Laurence LAFANECHERE
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CONTEXT
Most
of the emphasis in cancer therapy has been focused on primary
tumours. Most cancer deaths, however, are the result of metastatic
disease.
LIM Kinase is a signaling node that controls both
actin and microtubule dynamics. It has been identified has an enzyme whose
inhibition is supposed to stop the progression of invasive cancers. So far, however, few inhibitors have been
discovered, with poorly analyzed selectivity and no in vivo therapeutic efficacy described. The inventors have discovered of a new small-molecule inhibitors, highly
selective for LIM Kinase, which, when applied on cells stabilize microtubules
and suppress actin dynamics. These
inhibitors are effective not only in cancerous cell lines, including
Taxol®-resistant cell lines, but also in animals, where it delays tumors
formation while showing a good tolerability. It could represent a
pharmacological alternative to overcome the resistances often observed when tumors
are treated with microtubule targeting agents.
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