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Disease
Symptom
Drug
Enzyme
Compound
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Target Concepts:
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Query: EC:2.7.1.1 (
hexokinase
)
5,274
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Using a method of electrophoretic separation on agar gel, the
hexokinase
(HK) isoenzymes were determined in biopsies from patients with gastric and esophageal cancer and nonmalignant diseases (gastric benign tumors and gastritis) as well as in biopsies from healthy people. In the malignant neoplasms studied, a significant elevation of HK-II and the appearance of additional anodal bands (HK-IIf and HK-III) have been demonstrated. As a rule, the HK isoenzyme spectrum in gastric polyps was similar to that of normal mucosa and characterized by a predominance of HK-I. Changes in the HK isoenzyme composition in gastric mucosa with intestinal metaplasia were expressed in lesser degree but had similar cancerous tendency. The HK isoenzyme analysis in biopsy samples may be used for differential diagnosis of malignant and benign tumors, and/or as definite diagnostic implication of an early sign of
malignancy
in the study of premalignant lesions.
...
PMID:Hexokinase isoenzymes in the diagnosis of gastric and esophageal neoplasms. 361 66
The aerobic glycolysis rate and mitochondria-bound
hexokinase
activity of ascitic liver cancer cells are 8 and 50 times as high as those of the normal liver cells, and they can be inhibited by Na2SeO3 in concentration below 10 micrograms/ml. The inhibitory effect increases with selenium concentration. In contrast, Na2SeO3 at the same concentration does not significantly affect the glycolysis rate and mitochondria-bound
hexokinase
activity of the normal liver cells. The selective action of selenium on energy metabolism of the liver cancer cells may account for its inhibitory effect on
cancer
cells.
...
PMID:[Mechanism of the anticancer action of selenium--influence on glycolysis and its key enzyme]. 367 14
Serum levels of phosphohexose isomerase (PHI), aldolase (ALD) and
hexokinase
(HK) activities have been determined in 76 patients of carcinoma cervix, in search of proper diagnostic and prognostic parameters. All the three glycolytic enzyme levels studied were found to be significantly elevated in all the groups of
malignancy
and showed a relation to the clinical stage and tumor. Serum PHI levels were of best diagnostic significance even at an early stage of the disease. The enzyme levels correlated well with the prognosis of the disease.
...
PMID:Diagnostic and prognostic significance of serum phosphohexose isomerase, aldolase and hexokinase in carcinoma cervix. 381 45
In tumoral cells derived from the insulin-producing rat cell line RINm5F, both low- and high-Km glucose-phosphorylating enzymic activities were present. The
hexokinase
-like enzyme was inhibited by glucose 6-phosphate and displayed a greater affinity for but lower maximal velocity with alpha-D-glucose than beta-D-glucose. A comparable anomeric behavior of
hexokinase
was observed in breast cancer (MCF-7) and lymphocytic leukemia (P388) cells. Thus, the anomeric specificity of
hexokinase
in tumoral cells was not different from that recently characterized in normal mammalian cells.
Cancer
Res 1985 Dec
PMID:Anomeric specificity of hexokinase in rat, human, and murine tumor cells. 390 82
Lonidamine is a potent inhibitor of spermatogenesis and a hyperthermic sensitizer. The principal established locus of biochemical action of lonidamine is a selective inhibitory effect of the energy metabolism either in NAD-linked reactions in germ cell mitochondria, as well as the glycolytic metabolism of a variety of tumor cell lines by means of inhibition of mitochondrially bound
hexokinase
. We carried out in vivo tumor experiments to determine whether lonidamine when combined with radiation could potentiate the cytotoxic effects of radiation on two murine tumors. The combined effects of single acute lonidamine (100 mg/kg) and single dose X-irradiation were evaluated on the transplanted methylcholanthrene-induced fibrosarcoma in BALB/c mice and on the radiation-induced fibrosarcoma in C3H/He mice. The radiosensitizing effect by lonidamine was maximal when lonidamine was administered immediately prior to or after X-irradiation. The dose modifying factor of lonidamine is estimated to be 1.36 for methylcholanthrene-induced fibrosarcoma tumors and 1.25 for radiation-induced fibrosarcoma tumors. There was no disproportionately enhanced skin reaction following the combined treatments. The present results of the potentiating effects of radiation may be attributed, in part, to the findings of cell culture studies that lonidamine is a potent inhibitor of repair of potentially lethal damage.
Cancer
Res 1986 Mar
PMID:Potentiation of radiation effects on two murine tumors by lonidamine. 394 89
Hexokinase (ADP: D-hexose-6-phosphotransferase,
EC 2.7.1.1
) was studied in human thyroid carcinomas (n = 11), follicular adenomas (n = 32), and normal thyroid tissue (n = 21). The specific activity was significantly increased in carcinoma (0.163 +/- 0.083 U/mg protein) compared with normal tissue (0.030 +/- 0.010 U/mg protein) (P less than 0.001). Specific activities of follicular adenomas are rather heterogeneous, but when subdivided into three groups according to histopathologic criteria, a significant difference was found between follicular adenomas group I and II and follicular adenomas group III. A lesser cellular differentiation of adenomas is indicated by the lower degree or even absence of colloid production and follicle formation. A higher proliferation rate may be assumed on the grounds of the irregularities in outline, the often defective pseudocapsule, and signs of compression of the surrounding tissue. The highest specific activity in adenomas was found in the group with the highest proliferative activity, i.e., group III, whereas the lowest specific activities were found in adenomas with the lowest grade of proliferation, i.e., group I; the former was comparable with values found in carcinomas and the latter was comparable with values found in normal thyroid tissue. An interesting difference was found when the compartmentation of
hexokinase
was compared in carcinomas of different degree of differentiation. In papillary carcinomas a significantly lower proportion of
hexokinase
(HK) is present in the cytosol in comparison to follicular and undifferentiated carcinomas. In carcinomas more HK II and less HK I was found in comparison with normal thyroid tissue. In contrast
hexokinase
isozyme composition and compartmentation in adenomas were not different from normal thyroid tissue.
Cancer
1985 Apr 01
PMID:Determination and characterization of hexokinase in thyroid cancer and benign neoplasms. 397 45
The serum phosphohexose isomerase (PHI), aldolase and
hexokinase
activities have been determined in 36 patients of carcinoma ovary with different clinical stages and in 25 healthy normal female subjects. The serum PHI and
hexokinase
levels were significantly elevated (P less than .001) in all the stages of
malignancy
while serum aldolase was significantly elevated only in stages III and IV of
malignancy
. The enzyme levels showed statistically significant response to therapy in stage II patients. The mean values in patients with progression of the disease were not significantly different.
...
PMID:Significance of serum phosphohexose isomerase, hexokinase and aldolase in carcinoma ovary. 405 17
Some antitumor agents known to specifically inhibit certain tumor cell enzymes were examined for activity against glycolytic enzymes and growth of the insect trypanosomatid, Crithidia fasciculata. The cytoplasmic enzymes
hexokinase
, alpha-glycerophosphate dehydrogenase, malic dehydrogenase, and glucose-6-phosphate dehydrogenase were tested. Agaricic acid (2-hydroxy-1,2,3-nonadecane tricarboxylic acid) was highly inhibitory (50 to 100%) to malic and alpha-glycerophosphate dehydrogenases at approximately 3 x 10(-5)m; 2-(p-hydroxyphenyl)-2-phenylpropane (2 x 10(-4)m), and 5,6-dichloro-2-benzoxazolinone (5 x 10(-4)m) were less effective (50% inhibition) against them. The antiprotozoal agents primaquine (4 x 10(-4)m) and Melarsoprol (8 x 10(-4)m) were 30 to 40% inhibitory. Agaricic acid, 2-(p-hydroxyphenyl)-2-phenylpropane, and 5,6-dichloro-2-benzoxazolinone inhibited growth of Crithidia at less than 10(-4)m. Eight other test compounds from the
Cancer
Chemotherapy National Service Center (CCNSC) were not toxic to cell growth, although two (4-biphenylcarboxylic acid and 1-[p-chlorobenzyl]-2-ethyl-5-methyl-indole-3-acetic acid) inhibited Crithidia alpha-glycerophosphate dehydrogenase below 1 mm. All of the compounds used specifically inhibited
cancer
cell alpha-glycerophosphate dehydrogenase. The corresponding enzyme in pathogenic African trypanosomes is important in their terminal respiration. C. fasciculata may be useful in preliminary evaluation of chemotherapeutic agents as potential trypanocides.
...
PMID:Effects of some antitumor agents on growth and glycolytic enzymes of the flagellate Crithidia. 578 78
Increased activity of 6-phosphogluconate dehydrogenase was found in human colon tumors as compared to the adjacent unaffected mucosa. Glucose 1,6-diphosphate (Glc-1,6-P2), an endogenous potent regulator of glucose metabolism, markedly inhibited the activity of 6-phosphogluconate dehydrogenase (6-PGD) in extracts of the normal and malignant human colon. Glc-1,6-P2 also inhibited the activity of
hexokinase
in these extracts. The endogenous levels of Glc-1,6-P2 in the colon and tumors were measured. Since the pentose cycle can be inhibited by Glc-1,6-P2, means to increase endogenous levels of Glc-1,6-P2 or to introduce it into cells, might result in antitumor effects.
Cancer
Lett 1984 Jun
PMID:Inhibition of 6-phosphogluconate dehydrogenase by glucose 1,6-diphosphate in human normal and malignant colon extracts. 623 85
Mitochondria were isolated from whole homogenates of normal liver and Novikoff hepatomas using reorienting rate zonal centrifugation on sucrose gradients. The activities of several mitochondrial-specific enzymes and ultrastructure were compared in the two tissues. Our results indicate that cytochrome oxidase, lipoamide dehydrogenase, malate dehydrogenase, and succinate dehydrogenase activities are all higher in liver homogenates than in Novikoff hepatoma homogenates. Mitochondrial
hexokinase
, however, is much greater in the hepatoma than in liver. The activity of these enzymes in isolated mitochondria displayed a much different pattern. Both cytochrome oxidase and succinate dehydrogenase activities were higher in hepatoma mitochondria than in liver mitochondria. Lipoamide dehydrogenase and malate dehydrogenase, conversely, were higher in liver mitochondria. Hexokinase was found to be virtually absent in liver mitochondria but plentiful in hepatoma mitochondria. Ultrastructural studies have shown that the hepatoma mitochondria are much smaller in size, which results in a decreased rate of migration into the gradient. These studies have also shown that normal liver consists of predominantly "condensed" forms of mitochondria, whereas hepatoma contained a majority of "twisted" species. Experiments using 1% bovine serum albumin in the homogenization procedures and in the gradient have confirmed earlier observations that bovine serum albumin is essential for optimal isolation of neoplastic mitochondria.
Cancer
Res 1980 May
PMID:Characteristics of mitochondria isolated by rate zonal centrifugation from normal liver and Novikoff hepatomas. 624 94
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