2-Oxo-N-aryl-1, 2, 3, 4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase
…, KR Brimacombe, H Veith, JM Bougie, T Daniel…
文献索引：Walsh, Martin J.; Brimacombe, Kyle R.; Veith, Henrike; Bougie, James M.; Daniel, Thomas; Leister, William; Cantley, Lewis C.; Israelsen, William J.; Vander Heiden, Matthew G.; Shen, Min; Auld, Douglas S.; Thomas, Craig J.; Boxer, Matthew B. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 21 p. 6322 - 6327
Compared to normal differentiated cells, cancer cells have altered metabolic regulation to support biosynthesis and the expression of the M2 isozyme of pyruvate kinase (PKM2) plays an important role in this anabolic metabolism. While the M1 isoform is a highly active enzyme, the alternatively spliced M2 variant is considerably less active and expressed in tumors. While the exact mechanism by which decreased pyruvate kinase activity ...
