Bioorganic and Medicinal Chemistry Letters p. 2206 - 2210 (2008)
Update date:2022-08-04
Topics:
Thomas, Allen A.
Le Huerou
De Meese
Gunawardana, Indrani
Kaplan, Tomas
Romoff, Todd T.
Gonzales, Stephen S.
Condroski, Kevin
Boyd, Steven A.
Ballard, Josh
Bernat, Bryan
DeWolf, Walter
Han, May
Lee, Patrice
Lemieux, Christine
Pedersen, Robin
Pheneger, Jed
Poch, Greg
Smith, Darin
Sullivan, Francis
Weiler, Solly
Wright, S. Kirk
Lin, Jie
Brandhuber, Barb
Vigers, Guy
Tumor cells extensively utilize the pentose phosphate pathway for the synthesis of ribose. Transketolase is a key enzyme in this pathway and has been suggested as a target for inhibition in the treatment of cancer. In a pharmacodynamic study, nude mice with xenografted HCT-116 tumors were dosed with 1 ('N3′-pyridyl thiamine'; 3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride), an analog of thiamine, the co-factor of transketolase. Transketolase activity was almost completely suppressed in blood, spleen, and tumor cells, but there was little effect on the activity of the other thiamine-utilizing enzymes α-ketoglutarate dehydrogenase or glucose-6-phosphate dehydrogenase. Synthesis and SAR of transketolase inhibitors is described.
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