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Literature summary for 2.7.1.105 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

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

Cloned(Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
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]

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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

Organism UniProt Comment Textmining
Homo sapiens Q16875
-
-

Purification (Commentary)

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

Source Tissue

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

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
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)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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
-
?
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

Synonyms Comment Organism
PFKFB3
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
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