What is it about?
Glutamine addiction is a hallmark for cancer progression. Glutamine antagonism modulates cellular pathways to inhibit tumor growth. This article examines the perturbations of metabolites resulting from such glutamine antagonism and provides a fit-for-purpose method to quantify the most perturbed metabolite (FGAR) in tumor cells and plasma.
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Why is it important?
We show the efficacy of GA-607, a tumor targeted glutamine antagonist prodrug designed in our lab. We also present a method to accurately quantify FGAR, a metabolite of glutamine antagonism, that could be used as a valuable pharmacodynamic marker in clinical development of glutamine antagonist therapies.
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This page is a summary of: Glutamine Antagonist GA-607 Causes a Dramatic Accumulation of FGAR which can be used to Monitor Target Engagement, Current Drug Metabolism, August 2021, Bentham Science Publishers, DOI: 10.2174/1389200222666210831125041.
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