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.
Perspectives
While a lot of research is focused on developing novel drugs and therapies, very few methods are published to support the clinical translation of such therapeutics. This article not only identifies an important metabolite of glutamine antagonism, it also provides a robust method to measure this metabolite and thus would be a useful tool for all glutamine targeted therapies.
Dr. Sadakatali Gori
Johns Hopkins University
Read the Original
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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