BRENDA - Enzyme Database
show all sequences of 3.7.1.17

Mechanism-based inhibition of HsaD: a C-C bond hydrolase essential for survival of Mycobacterium tuberculosis in macrophage

Ryan, A.; Keany, S.; Eleftheriadou, O.; Ballet, R.; Cheng, H.Y.; Sim, E.; FEMS Microbiol. Lett. 350, 42-47 (2014)

Data extracted from this reference:

Cloned(Commentary)
Cloned (Commentary)
Organism
recombinant expression in Pseudomonas putida strain KT2442
Mycobacterium tuberculosis
Inhibitors
Inhibitors
Commentary
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
Commentary
Textmining
Mycobacterium tuberculosis
-
-
-
Purification (Commentary)
Purification (Commentary)
Organism
recombinant enzyme from Pseudomonas putida strain KT2442
Mycobacterium tuberculosis
Synonyms
Synonyms
Commentary
Organism
HsaD
-
Mycobacterium tuberculosis
Temperature Optimum [°C]
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
21
-
aassay at
Mycobacterium tuberculosis
pH Optimum
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
7.5
-
assay at
Mycobacterium tuberculosis
IC50 Value
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.63
-
pH 7.5, 21°C, recombinant enzyme
Mycobacterium tuberculosis
PMSF
Cloned(Commentary) (protein specific)
Commentary
Organism
recombinant expression in Pseudomonas putida strain KT2442
Mycobacterium tuberculosis
IC50 Value (protein specific)
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.63
-
pH 7.5, 21°C, recombinant enzyme
Mycobacterium tuberculosis
PMSF
Inhibitors (protein specific)
Inhibitors
Commentary
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
Purification (Commentary) (protein specific)
Commentary
Organism
recombinant enzyme from Pseudomonas putida strain KT2442
Mycobacterium tuberculosis
Temperature Optimum [°C] (protein specific)
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
21
-
aassay at
Mycobacterium tuberculosis
pH Optimum (protein specific)
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
7.5
-
assay at
Mycobacterium tuberculosis
Other publictions for EC 3.7.1.17
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Synonyms
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
733885
Ryan
Mechanism-based inhibition of ...
Mycobacterium tuberculosis
FEMS Microbiol. Lett.
350
42-47
2014
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14
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1
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14
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1
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1
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1
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717815
Lack
Characterization of a carbon-c ...
Mycobacterium tuberculosis
J. Biol. Chem.
285
434-443
2010
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1
1
1
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3
-
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1
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1
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3
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2
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4
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1
1
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3
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1
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3
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4
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3
3
717209
Lack
Temperature stability of prote ...
Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv
Biochem. J.
418
369-378
2009
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-
1
-
-
-
-
1
1
-
2
-
-
172
-
-
1
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-
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2
1
3
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1
1
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1
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1
1
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2
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1
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2
1
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1
1
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-
-
-
-
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-
1
1
717030
Lack
Structure of HsaD, a steroid-d ...
Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv
Acta Crystallogr. Sect. F
64
2-7
2007
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1
1
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-
-
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2
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172
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1
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1
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1
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1
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2
1
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718315
Van Der Geize
A gene cluster encoding choles ...
Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv
Proc. Natl. Acad. Sci. USA
104
1947-1952
2007
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1
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-
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1
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172
-
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4
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1
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1
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4
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654270
Horinouchi
A new bacterial steroid degrad ...
Comamonas testosteroni, Comamonas testosteroni TA441
Appl. Environ. Microbiol.
69
4421-4430
2003
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4
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2
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1
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2
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