Article
Characterization of the interactions of potent allosteric inhibitors with glutaminase C, a key enzyme in cancer cell glutamine metabolism.
The Journal of biological chemistry - 9 Mar 2018
Huang Qingqiu, Stalnecker Clint, Zhang Chengliang, McDermott Lee A, Iyer Prema, O'Neill Jason, Reimer Shawn, Cerione Richard A, Katt William P
Abstract excerpt
Altered glycolytic flux in cancer cells (the "Warburg effect") causes their proliferation to rely upon elevated glutamine metabolism ("glutamine addiction"). This requirement is met by the overexpression of glutaminase C (GAC), which catalyzes the first step in glutamine metabolism and therefore represents a potential therapeutic target. The small molecule CB-839 was reported to be more potent than other...
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