Literature summary for 2.2.1.1 extracted from

Thomas, A.A.; Le Huerou, Y.; De Meese, J.; Gunawardana, I.; Kaplan, T.; Romoff, T.T.; Gonzales, S.S.; Condroski, K.; Boyd, S.A.; Ballard, J.; Bernat, B.; DeWolf, W.; Han, M.; Lee, P.; Lemieux, C.; Pedersen, R.; Pheneger, J.; Poch, G.; Smith, D.; Sullivan, F.; Weiler, S.; Wright, S.K.; Lin, J.; Brandhuber, B.; Vigers, G.
Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors (2008), Bioorg. Med. Chem. Lett., 18, 2206-2210.

Application

Application	Comment	Organism
drug development	target for inhibition in the treatment of cancer	Homo sapiens

Inhibitors	Comment	Organism	Structure
3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride	analog of thiamine, almost completely suppresses transketolase activity in blood, spleen, and tumor cells, but has little effect on activity of the other thiamine-utilizing enzymes alpha-ketoglutarate dehydrogenase or glucose-6-phosphate dehydrogenase	Homo sapiens

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue	Comment	Organism	Textmining
blood	-	Homo sapiens	-
carcinoma cell	-	Homo sapiens	-
HCT-116 cell	-	Homo sapiens	-
spleen	-	Homo sapiens	-

Cofactor	Comment	Organism	Structure
thiamine diphosphate	-	Homo sapiens

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)