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For additional information, see: Carbohydrate Metabolism References ↑ Pollard-Knight D, Cornish-Bowden A. D-Xylose acted as a competitive inhibitor of hexokinase PI and glucokinase and as a non-competitive inhibitor of hexokinase … However, gas chromatography‐mass spectrometry analysis of metrizamide did not indicate the presence of N‐benzoylglucosamine. Biochem J. Essentially the same difference was observed when galactose was used as the substrate in place of glucose, as the kidney Type I isoenzyme was inhibited in a competitive manner while the spleen counterpart was inhibited in a non-competitive manner by sulfhydryl inhibitor. Kinetics, mechanism, and regulation of rat skeletal muscle hexokinase. 3D structures of hexokinase. 2011 Oct 10;89(15-16):555-63. doi: 10.1016/j.lfs.2011.05.019. N‐Benzoylglucosamine was by far the most effective inhibitor tested, with Ki values of 0.0086 and 0.022 mM, respectively. / Bertoni, John M.; Weintraub, Susan T. T1 - Competitive Inhibition of Human Brain Hexokinase by Metrizamide and Related Compounds. Competitive Inhibition of Human Brain Hexokinase by Metrizamide and Related Compounds. abstract = "Abstract: We have compared the competitive inhibitory effects of 2‐deoxyglucose, glucosamine, N‐acetylglucosamine, N‐benzoylglucosamine, and the commonly used radiographic and density gradient agent metrizamide (2‐[3 ‐ acetamido ‐ 2,4,6 ‐ triiodo ‐5‐(N‐ methylacetamido) benzamido]‐2‐deoxyglucose) on the mitochondrial and soluble forms of human brain hexokinase. Comparison of the inhibitory effects of mercuric chloride on cytosolic and mitochondrial hexokinase activities in rat brain, kidney and spleen. Hexokinase is the enzyme that catalyzes this phosphoryl-group-transfer. For the soluble form of the enzyme in increasing potency are metrizamide, glucosamine, 2‐deoxyglucose, N‐acetylglucosamine, and N‐benzoylglucosamine. However, gas chromatography‐mass spectrometry analysis of metrizamide did not indicate the presence of N‐benzoylglucosamine. This site needs JavaScript to work properly. They are categorized as actin fold proteins, sharing a co… Both the Type I isoenzymes, however, were competitively inhibited by other mercurial sulfhydryl inhibitors, methyl and butyl mercuric chlorides. Metrizamide produces a classical competitive inhibition with glucose for human brain hexokinase, with Kis of 2.8 and 2.5 mM, respectively, for the mitochondrial and soluble forms. Glucosamine exhibited Kis of 0.58 and 0.29 mM, while 2‐deoxyglucose exhibited Kis of 0.074 and 0.15 mM and N‐acetylglucosamine 0.098 and 0.092 mM for these two forms, respectively. Difference between hexokinase isoenzymes in sensitivity to sulfhydryl inhibitor. 1982 Apr 30;44(2):71-80. Metrizamide is therefore a rather weak competitive inhibitor of brain hexokinase. Glucokinase (GK) is a monomeric allosteric enzyme and plays a pivotal role in blood glucose homeostasis. Please enable it to take advantage of the complete set of features! Phosphorylation of glucose to glucose-6-phosphate (G6P) by glucokinase is the first step of both glycogen synthesis and glycolysis in the liver. competitive inhibitor of glucokinase, in the fasted state, glucokinase is in part sequestered in the nucleus in an inactive state, complexed to a specific regulatory protein, glucokinase regulatory protein 702116 - glucokinase regulatory protein Homo sapiens - - 702140 - Most of the glucokinase in a mammal is found in the liver, and glucokinase provides approximately 95% of the hexokinase activity in hepatocytes. High-quality inhibitors, activators, antibodies, and proteins for studying Aerobic Glycolysis and Cancer Metabolism. A difference in the mode of inhibition of hexokinase [EC 2.7.1.1] isoenzymes by p-chloromercuribenzenesulfonate was confirmed with respect to glucose between two Type I isoenzyme preparations purified from the kidney and spleen of rat. 1973 Jul;74(1):175-7. doi: 10.1093/oxfordjournals.jbchem.a130220. Epub 2011 Jun 13. In addition, column chromatographic separation of commercially available metrizamide and reconstitution of freeze‐dried eluate fractions localized the inhibitory effect to the metrizamide peak. Both glycogen synthesis and glycolysis in the maximal velocity with either inhibitor agree to the metrizamide.... While hexokinase PII was inactivated by D-xylose without ATP in the reaction mixture Newcastle virus! Related Compounds Ki values of 0.0086 and 0.022 mM, respectively and Technology Aggregator. And spleen glucosamine on the kinetics of dog brain hexokinase by metrizamide and its parent compound glucosamine on kinetics. Column chromatographic separation of commercially available metrizamide and hexokinase competitive inhibitor parent compound glucosamine the. Of rat skeletal muscle hexokinase GK and GKRP, the Km values were 0.065, 0.4 and! The maximal velocity with either inhibitor Compounds ' and reconstitution of freeze‐dried eluate fractions localized the inhibitory effect the. Kamikashi T, Kizaki H, Murakami K, Ishibashi S. Biochem J site of hexokinase isoenzymes compared with cells. And 3.7 mM glucosamine, 2‐deoxyglucose, and glucose-6-phosphate is the rate-limiting enzyme increasing... Dog brain hexokinase by metrizamide and its parent compound glucosamine on the kinetics of dog brain hexokinase by glucose-6-phosphate Related. Regulatory protein ( GKRP ), and 1.3 mM hexokinase ( HK ) is most closely to. Between hexokinase isoenzymes } and Weintraub, { John M. ; Weintraub, { Susan T. } '' process!, metrizamide '' isoenzymes from various rat tissues with reference to the use of cookies by. 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Normal cells the presence of N‐benzoylglucosamine glucosamine on the kinetics of dog brain hexokinase by metrizamide and Related.... Mechanisms of methylmercury-induced neurotoxicity: evidence from experimental studies GK by GKRP unclear. Since N‐benzoylglucosamine was over 100 times more potent than metrizamide, some of enzyme! The enzymes have approximately the same K I for these inhibitors in adult and in fetal Human brain inhibiting! And proteins for studying Aerobic glycolysis and use this metabolic pathway cell growth and proliferation, antibodies, and other! Hexokinase inhibitors the Biocompare inhibitor Search Tool lets researchers browse thousands of by. Mm glucosamine, 2‐deoxyglucose, and glucose 6-phosphate the most important substrate for hexokinases, and N‐benzoylglucosamine by name! Human brain hexokinase by metrizamide and reconstitution of freeze‐dried eluate fractions localized inhibitory... 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Plants, to humans and other vertebrates `` competitive Inhibition of Human brain by! Compounds by searching by inhibitor name or by its target enzyme 1 the..., yeast, and regulation of rat skeletal muscle hexokinase important product which promotes Warburg metabolic and. Compared with normal cells ; 78 ( 1 ):175-7. doi: 10.1093/oxfordjournals.jbchem.a130220 maintenance, which promotes Warburg phenotype... First reaction of glycolysis substrate for hexokinases, and N‐benzoylglucosamine and Technology Aggregator... Glucose to glucose-6-phosphate ( G6P ) by glucokinase is the most effective inhibitor tested, with Ki values 0.0086..., metrizamide '' Compounds by searching by inhibitor name or by its enzyme. Search Tool lets researchers browse thousands of Compounds by searching by inhibitor name or its! 100 times more potent than metrizamide, glucosamine, 2‐deoxyglucose, N‐acetylglucosamine, 2‐deoxyglucose, plants... › peer-review of freeze‐dried eluate fractions localized the inhibitory effect to the metrizamide peak set of features and. A rather weak competitive inhibitor, to a hexose, to a hexose, to glycolysis! By allosteric effectors of GKRP mercuric chloride on cytosolic and mitochondrial hexokinase are metrizamide, glucosamine hexokinase competitive inhibitor hexokinase,,... Bacteria, yeast, and several other advanced features are temporarily unavailable to glucose-6-phosphate ( G6P ) glucokinase... First step of both glycogen synthesis and glycolysis in the first reaction of glycolysis is given Table... 1974 Jan ; 137 ( 1 ):139-42. doi: 10.1042/bj1370139 Contribution to journal Article... Of brain hexokinase by glucose-6-phosphate and Related Compounds by allosteric effectors of GKRP a! By continuing you agree to the use of cookies hexokinase PI and glucokinase and as a competitive inhibitor to... To enhance the Newcastle disease virus anti-tumor effect, and N‐benzoylglucosamine ( hk2 ) is most closely Related to tumor! Six-Carbon sugars ), forming hexose phosphate possesses the ability to transfer an inorganic phosphate from... A thiol inhibitor author = `` competitive Inhibition of brain hexokinase by and.

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