Literature summary for 3.3.2.6 extracted from

Tholander, F.; Roques, B.P.; Fournie-Zaluski, M.C.; Thunnissen, M.M.; Haeggstroem, J.Z.
Crystal structure of leukotriene A4 hydrolase in complex with kelatorphan, implications for design of zinc metallopeptidase inhibitors (2010), FEBS Lett., 584, 3446-3451.

Cloned(Commentary)

Cloned (Comment)	Organism
expression in Escherichia coli	Homo sapiens

Crystallization (Commentary)

Crystallization (Comment)	Organism
in complex with inhibitor N-[3(R)-[(hydroxyamino)carbonyl]-2-benzyl-1-oxopropyl]-L-alanine, to 1.9 A resolution, space group P212121. The inhibitor binds along the sequence signature for M1 aminopeptidases, GXMEN. It exhibits bidentate chelation of the catalytic zinc and binds to LTA4H's enzymatically essential carboxylate recognition site. The inhibitor binds in an extended beta-sheet conformation between the zinc ion and Arg563. The carboxyl moiety forms two hydrogen bonds with Arg563, and the hydroxamate moiety chelates the zinc ion in a bidentate fashion	Homo sapiens

Crystallization (Comment)

Organism

in complex with inhibitor N-[3(R)-[(hydroxyamino)carbonyl]-2-benzyl-1-oxopropyl]-L-alanine, to 1.9 A resolution, space group P212121. The inhibitor binds along the sequence signature for M1 aminopeptidases, GXMEN. It exhibits bidentate chelation of the catalytic zinc and binds to LTA4H's enzymatically essential carboxylate recognition site. The inhibitor binds in an extended beta-sheet conformation between the zinc ion and Arg563. The carboxyl moiety forms two hydrogen bonds with Arg563, and the hydroxamate moiety chelates the zinc ion in a bidentate fashion

Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
N-[3(R)-[(hydroxyamino)carbonyl]-2-benzyl-1-oxopropyl]-L-alanine	i.e. kelatorphan, potent inhibitor of Zn-metalloenzymes	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P09960	-	-

Synonyms

Synonyms	Comment	Organism
LTA4H	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00017	-	pH 8.0, temperature not specified in the publication	Homo sapiens	N-[3(R)-[(hydroxyamino)carbonyl]-2-benzyl-1-oxopropyl]-L-alanine

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Release 2023.1 (January 2023)