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Literature summary for 3.1.1.4 extracted from

  • Burke, J.E.; Babakhani, A.; Gorfe, A.A.; Kokotos, G.; Li, S.; Woods, V.L.; McCammon, J.A.; Dennis, E.A.
    Location of inhibitors bound to group IVA phospholipase A2 determined by molecular dynamics and deuterium exchange mass spectrometry (2009), J. Am. Chem. Soc., 131, 8083-8091.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development possibilities of enhanced rational drug design against GIVA PLA2 through the powerful combination of experimental and computational work (deuterium exchange mass spectrometry and molecular dynamics simulation) synthetic construct

Cloned(Commentary)

Cloned (Comment) Organism
C-terminal His6-tagged GIVA PLA2 expressed using recombinant baculovirus in a suspension culture of Sf9 insect cells synthetic construct

Inhibitors

Inhibitors Comment Organism Structure
AX007 interacts with key residues that also exhibit changes in deuterium exchange upon inhibitor binding. Is bound mainly through contacts near the active site. Residues 481-495 and 543-553 exhibit an increase in exchange in the presence of the oxoamide, whereas 393-397 does not show any difference in exchange in the presence of the oxoamide in contrast to the inhibitor pyrrophenone synthetic construct
pyrrophenone interacts with key residues that also exhibit changes in deuterium exchange upon inhibitor binding. Is bound to the protein through numerous hydrophobic residues located distal from the active site. Residues 393-397, 481-495, and 543-553 exhibit increased rates of exchange in the presence of pyrrophenone synthetic construct

Organism

Organism UniProt Comment Textmining
synthetic construct
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-
-

Purification (Commentary)

Purification (Comment) Organism
by centrifugation and on nickel-nitrilotriacetic acid column synthetic construct

Storage Stability

Storage Stability Organism
0°C, 25 mM Tris-HCl buffer, pH 8.0, 100 mM NaCl, 125 mM imidazole, 2 mM dithiothreitol synthetic construct

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information activity assayed using mixed micelles in a modified Dole assay synthetic construct ?
-
?

Synonyms

Synonyms Comment Organism
GIVA PLA2
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synthetic construct
group IVA phospholipase A2
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synthetic construct