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Literature summary 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

Cloned(Commentary)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.7.1.17 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
3.7.1.17 3-phenyl-1H-2-benzopyran-1-one weak inhibition Mycobacterium tuberculosis
3.7.1.17 4-(2-aminoethyl)benzenesulfonyl fluoride weak inhibition Mycobacterium tuberculosis
3.7.1.17 4-amidinophenylmethanesulfonyl fluoride weak inhibition Mycobacterium tuberculosis
3.7.1.17 4-nitrophenyl-4-[bis(1,3-benzodioxol-5-yl)(hydroxy)methyl]piperidine-1-carboxylate covalent inhibitor Mycobacterium tuberculosis
3.7.1.17 6-carbamimidoylnaphthalen-2-yl 4-carbamimidamidobenzoate weak inhibition Mycobacterium tuberculosis
3.7.1.17 7-amino-4-chloro-3-methoxy-1H-2-benzopyran weak inhibition Mycobacterium tuberculosis
3.7.1.17 benzamidine weak inhibition Mycobacterium tuberculosis
3.7.1.17 eserine an acetylcholinesterase inhibitor Mycobacterium tuberculosis
3.7.1.17 leupeptin weak inhibition Mycobacterium tuberculosis
3.7.1.17 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
3.7.1.17 neostigmine an acetylcholinesterase inhibitor Mycobacterium tuberculosis
3.7.1.17 PMSF
-
 Mycobacterium tuberculosis
3.7.1.17 Trichlorfon an acetylcholinesterase inhibitor, weak inhibition Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
3.7.1.17 Mycobacterium tuberculosis
-
-
-

Purification (Commentary)

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

Synonyms

EC Number Synonyms Comment Organism
3.7.1.17 HsaD
-
 Mycobacterium tuberculosis

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.7.1.17 21
-
 aassay at Mycobacterium tuberculosis

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.7.1.17 7.5
-
 assay at Mycobacterium tuberculosis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.7.1.17 0.63
-
 pH 7.5, 21°C, recombinant enzyme Mycobacterium tuberculosis PMSF