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Study offers innovative profile of enzyme that aids tumor growth

specifically their small-molecule metabolite profiles-to begin to decipher the complex metabolic and signaling networks of cancer.

According to the study, one of the primary advantages of the functional proteomic technology employed (activity-based protein profiling) is that it can be used to identify inhibitors for uncharacterized enzymes like KIAA1363. Moreover, because inhibitors are screened against many enzymes in parallel, both potency and selectivity factors are assigned simultaneously.

The development of a selective inhibitor of KIAA1363 was possible due to the availability of an activity-based proteomics probe for this enzyme. Such probes are now available for many enzyme classes that participate in cell metabolism, so Cravatt suggests "a large swath of the enzyme proteome" could be addressed using the study's experimental strategy.

"The success of our study opens the door to assembling the full range of enzymes into both metabolic and signaling networks contributing to complex pathologies like cancer," Cravatt said. "This could lead to the discovery of new markers for diagnosis and targets for treatment."
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Source:Scripps Research Institute


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