Nature Publishes Pre-Clinical Data on an Inhibitor of a Novel Target Discovered by Millennium
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The Takeda Oncology Company has announced publication of an article describing the discovery of MLN4924a small molecule inhibitor of the NEDD8-Activating Enzyme (NAE) in the journal Nature.
NAE modulates the level of proteins critical for the regulation of cancer cell growth and survival pathways. Preclinical data show that MLN4924 inhibition of NAE function alters these important cancer pathways and results in cancer cell death.
Data published in Nature demonstrate that MLN4924 not only inhibits detectable NAE pathway function in cancer cells in vitro but also does the same in human tumor xenografts in murine models leading to tumor growth inhibition at doses and schedules that were well tolerated. MLN4924 represents the first small molecule inhibitor to specifically target this class of enzyme.
“The work described in the Nature article highlights Millennium’s leadership in protein homeostasis research and drug discovery. It is very gratifying to see this science support the transition of MLN4924 into clinical development,” said Joseph B. Bolen, Ph.D., Chief Scientific Officer, Millennium. “This work is characteristic of our approach to defining new cancer drug targets and translating this information into new types of potential cancer therapeutics.”
“These preclinical results demonstrate that MLN4924 has potential in treating various types of cancer by selectively inducing apoptosis in cancer cells in in vivo animal models and in vitro cell assays,” said Teresa A. Soucy, Ph.D., lead author of the paper and senior scientist at Millennium. “The safety profile of MLN4924 now is being studied in Phase I trials in patients with solid tumors or hematologic malignancies.”
NAE modulates the level of proteins critical for the regulation of cancer cell growth and survival pathways. Preclinical data show that MLN4924 inhibition of NAE function alters these important cancer pathways and results in cancer cell death.
Data published in Nature demonstrate that MLN4924 not only inhibits detectable NAE pathway function in cancer cells in vitro but also does the same in human tumor xenografts in murine models leading to tumor growth inhibition at doses and schedules that were well tolerated. MLN4924 represents the first small molecule inhibitor to specifically target this class of enzyme.
“The work described in the Nature article highlights Millennium’s leadership in protein homeostasis research and drug discovery. It is very gratifying to see this science support the transition of MLN4924 into clinical development,” said Joseph B. Bolen, Ph.D., Chief Scientific Officer, Millennium. “This work is characteristic of our approach to defining new cancer drug targets and translating this information into new types of potential cancer therapeutics.”
“These preclinical results demonstrate that MLN4924 has potential in treating various types of cancer by selectively inducing apoptosis in cancer cells in in vivo animal models and in vitro cell assays,” said Teresa A. Soucy, Ph.D., lead author of the paper and senior scientist at Millennium. “The safety profile of MLN4924 now is being studied in Phase I trials in patients with solid tumors or hematologic malignancies.”
