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Literature summary extracted from

  • Clem, B.; Telang, S.; Clem, A.; Yalcin, A.; Meier, J.; Simmons, A.; Rasku, M.A.; Arumugam, S.; Dean, W.L.; Eaton, J.; Lane, A.; Trent, J.O.; Chesney, J.
    Small-molecule inhibition of 6-phosphofructo-2-kinase activity suppresses glycolytic flux and tumor growth (2008), Mol. Cancer Ther., 7, 110-120.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.1.105 medicine clinical development of PFKFB3 inhibitors as chemotherapeutic agents Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.105 subcloned into the pET-30b(+) vector, expression in BL21 (DE3) Escherichia coli Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.105 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one (3PO), small-molecule inhibitor, mixed inhibition mechanism, both competitive and uncompetitive inhibition, suppresses glycolytic flux and is cytostatic to neoplastic cells, inhibits activity of recombinantly expressed PFKFB3 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.1.105 0.097
-
 beta-D-fructose 6-phosphate
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.105 ATP + beta-D-fructose 6-phosphate Homo sapiens PFKFB3 is a potent stimulator of glycolysis, up-regulated by inflammatory and hypoxic stimuli ADP + beta-D-fructose 2,6-bisphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.105 Homo sapiens Q16875
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.1.105 gel filtration, recombinant protein Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.1.105 JURKAT cell engineered to overexpress PFKFB3, inhibitor studies on recombinant PFKFB3 activity in Homo sapiens
-
2.7.1.105 leukemia cell constitutively expressed in Homo sapiens
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.7.1.105 0.277
-
 specific PFK-2 activity of the recombinant PFKFB3 protein determined by measurement of fructose 2,6-bisphosphate Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.105 ATP + beta-D-fructose 6-phosphate PFKFB3 is a potent stimulator of glycolysis, up-regulated by inflammatory and hypoxic stimuli Homo sapiens ADP + beta-D-fructose 2,6-bisphosphate
-
 ?
2.7.1.105 ATP + beta-D-fructose 6-phosphate PFKFB3 is a potent stimulator of glycolysis, up-regulated by inflammatory and hypoxic stimuli, role in the progression of cancerous cells, antiproliferative effects during inhibitor incubation determined Homo sapiens ADP + beta-D-fructose 2,6-bisphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.105 PFKFB3
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.1.105 0.025
-
 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one inhibition of recombinant PFKFB3 protein, no inhibition of purified PFK-1 activity Homo sapiens