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Literature summary for 3.4.21.105 extracted from

  • Wolf, E.V.; Zeissler, A.; Verhelst, S.H.
    Inhibitor fingerprinting of rhomboid proteases by activity-based protein profiling reveals inhibitor selectivity and rhomboid autoprocessing (2015), ACS Chem. Biol., 10, 2325-2333 .
    View publication on PubMed
Search for more literature for 3.4.21.105

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Escherichia coli
expression in Escherichia coli Providencia stuartii
expression in Escherichia coli Vibrio cholerae

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with covalently bound inhibitor 3-butyl-4-(pent-4-yn-1-yl)oxetan-2-one Escherichia coli

Protein Variants

Protein Variants Comment Organism
S150A active site mutant. In contrast to the wild-type, only a band of 33000 Da is seen on SDS-PAGE Providencia stuartii
S150A active site mutant. In contrast to the wild-type, only a band of 33000 Da is seen on SDS-PAGE Vibrio cholerae

Inhibitors

Inhibitors Comment Organism Structure
3-butyl-4-(pent-4-yn-1-yl)oxetan-2-one
-
 Escherichia coli
4-chloro-7-nitro-3-[(5-phenylpentyl)oxy]-1H-2-benzopyran-1-one inhibitor reacts with virtually all tested rhomboids Escherichia coli
additional information comparison of the inhibitory capacity of 50 small molecules against 13 different rhomboids unsing activity-based protein profiling. Inhibition profile and sequence similarity of rhomboids are not related, which suggests that related rhomboids may be selectively inhibited Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli P09391
-
-
Providencia stuartii P46116
-
-
Vibrio cholerae
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification AarA undergoes N-terminal processing Providencia stuartii
proteolytic modification protein undergoes N-terminal processing Vibrio cholerae

Subunits

Subunits Comment Organism
? x * 3000, and x* 33000, SDS-PAGE Providencia stuartii
? x * 31000, SDS-PAGE. Upon incubation of enzyme at 37 °C, lower species start to occur Vibrio cholerae

Synonyms

Synonyms Comment Organism
AarA
-
 Providencia stuartii
AarA
-
 Vibrio cholerae
GlpG
-
 Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.044
-
 pH not specified in the publication, temperature not specified in the publication Escherichia coli 3-butyl-4-(pent-4-yn-1-yl)oxetan-2-one