EC Number |
Inhibitors |
Structure |
---|
2.2.1.1 | 1-(3-chloro-2-methylphenyl)-3-(2-hydroxy-5-nitrophenyl)urea |
inhibitor designed to cover a hot spot in the dimerization interface of the homodimer of the enzyme |
|
2.2.1.1 | 1-(5-chloro-2-hydroxy-4-nitrophenyl)-3-phenylurea |
inhibitor designed to cover a hot spot in the dimerization interface of the homodimer of the enzyme |
|
2.2.1.1 | 1-(5-hydroxynaphthalen-1-yl)-3-(2-methyl-5-nitrophenyl)urea |
inhibitor designed to cover a hot spot in the dimerization interface of the homodimer of the enzyme |
|
2.2.1.1 | 2-[(2,2-dimethyl-2,3-dihydro-1-benzofuran-7-yl)oxy]-N-[1-(4-ethyl-6-hydroxypyrimidin-2-yl)-4-(furan-2-yl)-1H-pyrrol-2-yl]acetamide |
- |
|
2.2.1.1 | 3-(2,4-dichlorophenoxy)-N-[3-(furan-2-yl)-1-(pyrimidin-2-yl)-1H-pyrazol-5-yl]propanamide |
- |
|
2.2.1.1 | 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 |
|
2.2.1.1 | 3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride |
analog of thiamine, potent transketolase inhibitor but suffers from poor pharmacokinetics due to high clearance and Cmax linked toxicity. Efficient way of improving the pharmacokinetic profile is to prepare oxidized prodrugs which are slowly reduced in vivo yielding longer, sustained blood levels of the drug |
|
2.2.1.1 | 3-formylbenzoic acid |
substrate inhibition |
|
2.2.1.1 | 4'-methylamino-thiamine diphosphate |
cofactor analogue |
|
2.2.1.1 | ADP |
- |
|