Literature summary for 1.3.1.9 extracted from

Maity, K.; Banerjee, T.; Prabakaran, N.; Surolia, N.; Surolia, A.; Suguna, K.
Effect of substrate binding loop mutations on the structure, kinetics, and inhibition of enoyl acyl carrier protein reductase from Plasmodium falciparum (2011), IUBMB Life, 63, 30-41.

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Cloned(Commentary)

Cloned (Comment)	Organism
expression in Escherichia coli	Plasmodium falciparum

Crystallization (Commentary)

Crystallization (Comment)	Organism
mutants A372M, K316A in cimolex with triclosan, to 2.5 and 2.05 A resolution, respectively. The enzyme has a conserved salt bridge which stabilizes the substrate binding loop and appears to be important for the active conformation	Plasmodium falciparum

Protein Variants

Protein Variants	Comment	Organism
A372M	mutation increases the affinity of the enzyme towards triclosan to almost double	Plasmodium falciparum
A372V	mutation increases the affinity of the enzyme towards triclosan to almost double	Plasmodium falciparum
A372V/K316A	enzymatically inactive	Plasmodium falciparum
A372V/K316E	enzymatically inactive	Plasmodium falciparum
D370A	enzymatically inactive	Plasmodium falciparum
D370K	enzymatically inactive	Plasmodium falciparum
K316A	no change in affinity to triclosan	Plasmodium falciparum
K316E	enzymatically inactive	Plasmodium falciparum
K316I	enzymatically inactive	Plasmodium falciparum

Inhibitors

Inhibitors	Comment	Organism	Structure
triclosan	competitive with NADH, uncompetitive with NAD+	Plasmodium falciparum

Organism

Organism	UniProt	Comment	Textmining
Plasmodium falciparum	Q9BJJ9	-	-

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.000025	-	triclosan	wild-type, substrate NADH, pH not specified in the publication, temperature not specified in the publication	Plasmodium falciparum
0.000028	-	triclosan	wild-type, substrate NAD+, pH not specified in the publication, temperature not specified in the publication	Plasmodium falciparum

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000033	-	mutant A372V, pH not specified in the publication, temperature not specified in the publication	Plasmodium falciparum	triclosan
0.000035	-	mutant A372M, pH not specified in the publication, temperature not specified in the publication	Plasmodium falciparum	triclosan
0.000066	-	wild-type, pH not specified in the publication, temperature not specified in the publication	Plasmodium falciparum	triclosan
0.000066	-	mutant K316A, pH not specified in the publication, temperature not specified in the publication	Plasmodium falciparum	triclosan

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Release 2023.1 (January 2023)