Competitive Inhibition of Rat Brain Hexokinase by 2‐Deoxyglucose, Glucosamine, and Metrizamide

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

Abstract: The effects of metrizamide on the kinetics of rat brain hexokinase were compared in vitro with those of 2‐deoxyglucose and glucosamine. Although metrizamide, 2‐deoxyglucose, and glucosamine are known to be competitive inhibitors of approximately equal potency for glucose of yeast hexokinase (K1 approximately 0.7 mm for all three), metrizamide is a much weaker competitive inhibitor (Ki about 20 mm) of rat brain hexokinase than either 2‐deoxyglucose or glucosamine (Ki about 0.3 mm for both). This indicates a greater active site specificity of rat brain hexokinase than of yeast hexokinase. Rat brain hexokinase activity is enhanced approximately threefold in the presence of 0.05, 0.2, and 0.8 mg/ml bovine serum albumin, while yeast hexokinase is only enhanced by 50% under these conditions. Despite the high Ki value for metrizamide, interference with glucose metabolism may occur whenever metrizamide is present in much higher concentrations than glucose. Myelography in humans is one such situation.

Original languageEnglish (US)
Pages (from-to)1523-1528
Number of pages6
JournalJournal of Neurochemistry
Volume37
Issue number6
DOIs
StatePublished - Dec 1981

Fingerprint

Metrizamide
Hexokinase
Glucosamine
Rats
Brain
Yeast
Yeasts
Glucose
Myelography
Bovine Serum Albumin
Metabolism
Catalytic Domain
Kinetics

Keywords

  • 2‐Deoxyglucose
  • Brain
  • Glucosamine
  • Hexokinase
  • Inhibitor
  • Metrizamide

ASJC Scopus subject areas

  • Biochemistry
  • Cellular and Molecular Neuroscience

Cite this

Competitive Inhibition of Rat Brain Hexokinase by 2‐Deoxyglucose, Glucosamine, and Metrizamide. / Bertoni, John M.

In: Journal of Neurochemistry, Vol. 37, No. 6, 12.1981, p. 1523-1528.

Research output: Contribution to journalArticle

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abstract = "Abstract: The effects of metrizamide on the kinetics of rat brain hexokinase were compared in vitro with those of 2‐deoxyglucose and glucosamine. Although metrizamide, 2‐deoxyglucose, and glucosamine are known to be competitive inhibitors of approximately equal potency for glucose of yeast hexokinase (K1 approximately 0.7 mm for all three), metrizamide is a much weaker competitive inhibitor (Ki about 20 mm) of rat brain hexokinase than either 2‐deoxyglucose or glucosamine (Ki about 0.3 mm for both). This indicates a greater active site specificity of rat brain hexokinase than of yeast hexokinase. Rat brain hexokinase activity is enhanced approximately threefold in the presence of 0.05, 0.2, and 0.8 mg/ml bovine serum albumin, while yeast hexokinase is only enhanced by 50{\%} under these conditions. Despite the high Ki value for metrizamide, interference with glucose metabolism may occur whenever metrizamide is present in much higher concentrations than glucose. Myelography in humans is one such situation.",
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N2 - Abstract: The effects of metrizamide on the kinetics of rat brain hexokinase were compared in vitro with those of 2‐deoxyglucose and glucosamine. Although metrizamide, 2‐deoxyglucose, and glucosamine are known to be competitive inhibitors of approximately equal potency for glucose of yeast hexokinase (K1 approximately 0.7 mm for all three), metrizamide is a much weaker competitive inhibitor (Ki about 20 mm) of rat brain hexokinase than either 2‐deoxyglucose or glucosamine (Ki about 0.3 mm for both). This indicates a greater active site specificity of rat brain hexokinase than of yeast hexokinase. Rat brain hexokinase activity is enhanced approximately threefold in the presence of 0.05, 0.2, and 0.8 mg/ml bovine serum albumin, while yeast hexokinase is only enhanced by 50% under these conditions. Despite the high Ki value for metrizamide, interference with glucose metabolism may occur whenever metrizamide is present in much higher concentrations than glucose. Myelography in humans is one such situation.

AB - Abstract: The effects of metrizamide on the kinetics of rat brain hexokinase were compared in vitro with those of 2‐deoxyglucose and glucosamine. Although metrizamide, 2‐deoxyglucose, and glucosamine are known to be competitive inhibitors of approximately equal potency for glucose of yeast hexokinase (K1 approximately 0.7 mm for all three), metrizamide is a much weaker competitive inhibitor (Ki about 20 mm) of rat brain hexokinase than either 2‐deoxyglucose or glucosamine (Ki about 0.3 mm for both). This indicates a greater active site specificity of rat brain hexokinase than of yeast hexokinase. Rat brain hexokinase activity is enhanced approximately threefold in the presence of 0.05, 0.2, and 0.8 mg/ml bovine serum albumin, while yeast hexokinase is only enhanced by 50% under these conditions. Despite the high Ki value for metrizamide, interference with glucose metabolism may occur whenever metrizamide is present in much higher concentrations than glucose. Myelography in humans is one such situation.

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