Journal
FUTURE MEDICINAL CHEMISTRY
Volume 9, Issue 2, Pages 223-243Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2016-0190
Keywords
968; BPTES; cancer; CB-839; glutaminase; inhibitor; metabolism; Warburg effect
Categories
Funding
- NIH [GM040654, GM047458, CA201402]
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Many cancer cells exhibit an altered metabolic phenotype, in which glutamine consumption is upregulated relative to healthy cells. This metabolic reprogramming often depends upon mitochondrial glutaminase activity, which converts glutamine to glutamate, a key precursor for biosynthetic and bioenergetic processes. Two isozymes of glutaminase exist, a kidney-type (GLS) and a liver-type enzyme (GLS2 or LGA). While a majority of studies have focused on GLS, here we summarize key findings on both glutaminases, describing their structure and function, their roles in cancer and pharmacological approaches to inhibiting their activities.
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