Small Molecules to Perturb A Novel PPI Target For Chemotherapy
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abstract
Acute myeloid leukemia (AML) is a prevalent and aggressive form of blood cancer with a poor prognosis, particularly for older people. Most of the established drugs to treat AML are horribly toxic. However, some emerging treatments are likely to be better tolerated because they target a particular biochemical pathway that is switched on in cancer cells, making them more vulnerable to the drug than healthy ones. One such drug candidate in clinical trials, MLN4924, is unique insofar as it modifies a protein called NAE so that it is no longer able to bind to another one called NEDD8. Clinical data for MLN4924 is extremely promising, but cell studies indicate some forms of AML could be resistant.... Read More Acute myeloid leukemia (AML) is a prevalent and aggressive form of blood cancer with a poor prognosis, particularly for older people. Most of the established drugs to treat AML are horribly toxic. However, some emerging treatments are likely to be better tolerated because they target a particular biochemical pathway that is switched on in cancer cells, making them more vulnerable to the drug than healthy ones. One such drug candidate in clinical trials, MLN4924, is unique insofar as it modifies a protein called NAE so that it is no longer able to bind to another one called NEDD8. Clinical data for MLN4924 is extremely promising, but cell studies indicate some forms of AML could be resistant. Consequently, it is highly desirable to explore compounds with the potential to prevent NAE interacting with NEDD8 in a different way, and that is the focus of the proposed study..........
