Grant ID RP240320
Awarded On February 21, 2024
Title Benzothiazepines as first-in-class inhibitors for the ribogenesis factor NVL and evaluation in preclinical colorectal cancer models
Program Academic Research
Award Mechanism Individual Investigator
Institution/Organization The University of Texas Southwestern Medical Center
Principal Investigator/Program Director Jef K De Brabander
Cancer Sites Colorectal
Contracted Amount $1,049,754
Lay Summary

Oxaliplatin, a frontline agent for colorectal cancer (CRC) treatment, has a mechanism of action that differs from other platinum drugs by blocking ribosome biogenesis rather than DNA damage. The target of oxaliplatin that induces ribosome biogenesis is not known. In spite of its clinical benefit, oxaliplatin has numerous adverse events and is often dose limited. Nonetheless, the preferential use of oxaliplatin in CRC raises the hypothesis that more specific and targeted inhibitors of ribosome biogenesis may be better tolerated and benefit patients with CRC. We discovered a novel molecule (MM017) with potent activity against CRC that specifically targets a factor required for ribosome biogene...

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