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Literature summary for 2.3.1.97 extracted from

  • Fang, W.; Robinson, D.A.; Raimi, O.G.; Blair, D.E.; Harrison, J.R.; Lockhart, D.E.; Torrie, L.S.; Ruda, G.F.; Wyatt, P.G.; Gilbert, I.H.; van Aalten, D.M.
    N-myristoyltransferase is a cell wall target in Aspergillus fumigatus (2015), ACS Chem. Biol., 10, 1425-1434.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Aspergillus fumigatus

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitors 2,6-dichloro-4-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-N-(1,5-dimethyl-3-isobutyl-1H-pyrazol-4-yl)benzenesulfonamide and 2,6-dichloro-4-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide binding in the peptide substrate pocket Aspergillus fumigatus

Inhibitors

Inhibitors Comment Organism Structure
2,6-dichloro-4-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-N-(1,5-dimethyl-3-isobutyl-1H-pyrazol-4-yl)benzenesulfonamide inhibits the enzyme and is fungicidal under partially repressive nmt conditions Aspergillus fumigatus
2,6-dichloro-4-[2-(piperazin-1-yl)pyridin-4-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide
-
Aspergillus fumigatus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0008
-
myristoleoyl-CoA pH not specified in the publication, temperature not specified in the publication Aspergillus fumigatus
0.022
-
CAP5.5 pH not specified in the publication, temperature not specified in the publication Aspergillus fumigatus

Localization

Localization Comment Organism GeneOntology No. Textmining

Organism

Organism UniProt Comment Textmining
Aspergillus fumigatus Q9UVX3
-
-
Aspergillus fumigatus ATCC MYA-4609 Q9UVX3
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
myristoleoyl-CoA + CAP5.5 acceptor is biotin-tagged cytoskeleton-associated protein 5.5 Aspergillus fumigatus N-myristoleoyl-CAP5.5 + CoA
-
?
myristoleoyl-CoA + CAP5.5 acceptor is biotin-tagged cytoskeleton-associated protein 5.5 Aspergillus fumigatus ATCC MYA-4609 N-myristoleoyl-CAP5.5 + CoA
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000012
-
pH not specified in the publication, temperature not specified in the publication Aspergillus fumigatus 2,6-dichloro-4-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-N-(1,5-dimethyl-3-isobutyl-1H-pyrazol-4-yl)benzenesulfonamide
0.000023
-
pH not specified in the publication, temperature not specified in the publication Aspergillus fumigatus 2,6-dichloro-4-[2-(piperazin-1-yl)pyridin-4-yl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)benzenesulfonamide

General Information

General Information Comment Organism
physiological function expression of the Nmt gene is essential for viability. Partial repression of the gene reveals downstream effects of N-myristoylation on cell wall morphology Aspergillus fumigatus