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Literature summary for 3.7.1.17 extracted from

  • Ryan, A.; Keany, S.; Eleftheriadou, O.; Ballet, R.; Cheng, H.Y.; Sim, E.
    Mechanism-based inhibition of HsaD: a C-C bond hydrolase essential for survival of Mycobacterium tuberculosis in macrophage (2014), FEMS Microbiol. Lett., 350, 42-47.
    View publication on PubMed
Search for more literature for 3.7.1.17

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression in Pseudomonas putida strain KT2442 Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
3,4-dichloroisocoumarin a broad spectrum covalent inhibitor of serine proteases, the structural homologues of 3,4-dichloroisocoumarin, 7-amino-4-chloro-3-methoxy-1H-2-benzopyran and 3-phenyl-1H-2-benzopyran-1-one, show significantly poorer inhibition Mycobacterium tuberculosis
3-phenyl-1H-2-benzopyran-1-one weak inhibition Mycobacterium tuberculosis
4-(2-aminoethyl)benzenesulfonyl fluoride weak inhibition Mycobacterium tuberculosis
4-amidinophenylmethanesulfonyl fluoride weak inhibition Mycobacterium tuberculosis
4-nitrophenyl-4-[bis(1,3-benzodioxol-5-yl)(hydroxy)methyl]piperidine-1-carboxylate covalent inhibitor Mycobacterium tuberculosis
6-carbamimidoylnaphthalen-2-yl 4-carbamimidamidobenzoate weak inhibition Mycobacterium tuberculosis
7-amino-4-chloro-3-methoxy-1H-2-benzopyran weak inhibition Mycobacterium tuberculosis
benzamidine weak inhibition Mycobacterium tuberculosis
eserine an acetylcholinesterase inhibitor Mycobacterium tuberculosis
leupeptin weak inhibition Mycobacterium tuberculosis
additional information inhibition of HsaD by serine protease inhibitors. No inhibition by acetylcholinesterase inhibitors edrophonium, tacrine, and pyridostigmine. Consistent with the lack of a cysteine residue in the active site of HsaD, covalent inhibitor nicotinamide does not significantly inhibit HsaD Mycobacterium tuberculosis
neostigmine an acetylcholinesterase inhibitor Mycobacterium tuberculosis
PMSF
-
 Mycobacterium tuberculosis
Trichlorfon an acetylcholinesterase inhibitor, weak inhibition Mycobacterium tuberculosis

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzyme from Pseudomonas putida strain KT2442 Mycobacterium tuberculosis

Synonyms

Synonyms Comment Organism
HsaD
-
 Mycobacterium tuberculosis

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
21
-
 aassay at Mycobacterium tuberculosis

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Mycobacterium tuberculosis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.63
-
 pH 7.5, 21°C, recombinant enzyme Mycobacterium tuberculosis PMSF