Article
Structural basis for the allosteric inhibitory mechanism of human kidney-type glutaminase (KGA) and its regulation by Raf-Mek-Erk signaling in cancer cell metabolism.
Proceedings of the National Academy of Sciences of the United States of America - 15 May 2012
Thangavelu K, Pan Catherine Qiurong, Karlberg Tobias, Balaji Ganapathy, Uttamchandani Mahesh, Suresh Valiyaveettil, Schüler Herwig, Low Boon Chuan, Sivaraman J
Abstract excerpt
Besides thriving on altered glucose metabolism, cancer cells undergo glutaminolysis to meet their energy demands. As the first enzyme in catalyzing glutaminolysis, human kidney-type glutaminase isoform (KGA) is becoming an attractive target for small molecules such as BPTES [bis-2-(5 phenylacetamido-1, 2, 4-thiadiazol-2-yl) ethyl sulfide], although the regulatory mechanism of KGA remains unknown. On the basis of...
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