BRENDA - Enzyme Database

Bacterial Peptide deformylase inhibitors: a new class of antibacterial agents

Jain, R.; Chen, D.; White, R.J.; Patel, D.V.; Yuan, Z.; Curr. Med. Chem. 12, 1607-1621 (2005)

Data extracted from this reference:

Application
EC Number
Application
Commentary
Organism
3.5.1.88
medicine
target for the development of new antibacterial drugs
Haemophilus influenzae
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
3.5.1.88
2-oxo-pyrrolidine with chelators
-
Haemophilus influenzae
3.5.1.88
2-thioxo-4-thiazolidinone N-hexanoic acid
IC50 against Escherichia coli peptide deformylase: 0.00166 mM
Haemophilus influenzae
3.5.1.88
actinonin
IC50 against Escherichia coli peptide deformylase: 0.0000003 mM
Haemophilus influenzae
3.5.1.88
aldehyde peptide
IC50 against Escherichia coli peptide deformylase: 0.01 mM
Haemophilus influenzae
3.5.1.88
alkyl-succinate-proline hydroxamate
IC50 against Escherichia coli peptide deformylase: 0.000004-0.000010 mM
Haemophilus influenzae
3.5.1.88
benzimidazole N-formyl hydroxylamine
-
Haemophilus influenzae
3.5.1.88
benzothiazinone derivatives
IC50: 0.000005 mM
Haemophilus influenzae
3.5.1.88
benzothiazolylidene hydroxamic acid derivatives
IC50 against Escherichia coli peptide deformylase: 0.00104 mM
Haemophilus influenzae
3.5.1.88
beta-sulfonylhydroxamic acid
IC50 against Escherichia coli peptide deformylase: 0.000016 mM
Haemophilus influenzae
3.5.1.88
carbamate N-formyl hydroxylamine
-
Haemophilus influenzae
3.5.1.88
heteroarylaryl(P2'/P3')N-formyl hydroxylamine
-
Haemophilus influenzae
3.5.1.88
hydantoin
IC50 against Escherichia coli peptide deformylase: 0.0002 mM
Haemophilus influenzae
3.5.1.88
hydrazide N-formyl hydroxylamine
-
Haemophilus influenzae
3.5.1.88
isoxazole-3-hydroxamic acid derivatives
IC50 against Escherichia coli peptide deformylase: 0.0034 mM
Haemophilus influenzae
3.5.1.88
N-alkyl urea hydroxamate
IC50 against Escherichia coli peptide deformylase: 0.000003 mM
Haemophilus influenzae
3.5.1.88
N-hydroxy urea
IC50 against Escherichia coli peptide deformylase: 0.0022 mM
Haemophilus influenzae
3.5.1.88
N-hydroxy-2-(substituted phenyl) acetamide
-
Haemophilus influenzae
3.5.1.88
N-hydroxy-N-(3-hydrazino-3-oxopropyl)formamide
-
Haemophilus influenzae
3.5.1.88
N-substituted methionine hydrazide
IC50 against Escherichia coli peptide deformylase: 0.2 mM
Haemophilus influenzae
3.5.1.88
N-sulfonyl-L-Val-L-Leu-hydroxamate
-
Haemophilus influenzae
3.5.1.88
pseudopeptide metabolites
IC50 against Escherichia coli peptide deformylase: 0.000030 mM
Haemophilus influenzae
3.5.1.88
pyrrolidine bicyclic(P2'/P3')compounds
-
Haemophilus influenzae
3.5.1.88
quinazoline hydroxamic acid
IC50 against Escherichia coli peptide deformylase: 0.00012 mM
Haemophilus influenzae
3.5.1.88
thio peptide
IC50 against Escherichia coli peptide deformylase: 0.000019 mM, thiol chelating group combined with the best substrate motif
Haemophilus influenzae
3.5.1.88
thiol peptide
IC50 against Escherichia coli peptide deformylase: 0.0025 mM, designed based on the best substrate identified
Haemophilus influenzae
3.5.1.88
thyropropic acid derivatives
IC50 against Escherichia coli peptide deformylase: 0.001 mM
Haemophilus influenzae
3.5.1.88
urea analogs(P2'/P3')of N-formyl hydroxylamine
-
Haemophilus influenzae
Metals/Ions
EC Number
Metals/Ions
Commentary
Organism
Structure
3.5.1.88
Fe2+
-
Haemophilus influenzae
3.5.1.88
Ni2+
-
Haemophilus influenzae
3.5.1.88
Zn2+
-
Haemophilus influenzae
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.5.1.88
formyl-L-methionyl peptide + H2O
Haemophilus influenzae
-
formate + methionyl peptide
-
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
3.5.1.88
Haemophilus influenzae
-
-
-
Oxidation Stability
EC Number
Oxidation Stability
Organism
3.5.1.88
ferrous ion in peptide deformylase is very unstable and is quickly and irreversibly oxidized to the ferric ion under laboratory conditions, resulting in an inactive enzyme.
Haemophilus influenzae
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.5.1.88
formyl-L-methionyl peptide + H2O
-
673200
Haemophilus influenzae
formate + methionyl peptide
-
-
-
?
IC50 Value
EC Number
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
3.5.1.88
0.0000003
-
IC50 against Escherichia coli peptide deformylase: 0.0000003 mM
Haemophilus influenzae
actinonin
3.5.1.88
0.000003
-
IC50 against Escherichia coli peptide deformylase: 0.000003 mM
Haemophilus influenzae
N-alkyl urea hydroxamate
3.5.1.88
0.000004
0.00001
IC50 against Escherichia coli peptide deformylase: 0.000004-0.000010 mM
Haemophilus influenzae
alkyl-succinate-proline hydroxamate
3.5.1.88
0.000005
-
IC50: 0.000005 mM
Haemophilus influenzae
benzothiazinone derivatives
3.5.1.88
0.000016
-
IC50 against Escherichia coli peptide deformylase: 0.000016 mM
Haemophilus influenzae
beta-sulfonylhydroxamic acid
3.5.1.88
0.000019
-
IC50 against Escherichia coli peptide deformylase: 0.000019 mM, thiol chelating group combined with the best substrate motif
Haemophilus influenzae
thio peptide
3.5.1.88
0.00003
-
IC50 against Escherichia coli peptide deformylase: 0.000030 mM
Haemophilus influenzae
pseudopeptide metabolites
3.5.1.88
0.00012
-
IC50 against Escherichia coli peptide deformylase: 0.00012 mM
Haemophilus influenzae
quinazoline hydroxamic acid
3.5.1.88
0.0002
-
IC50 against Escherichia coli peptide deformylase: 0.0002 mM
Haemophilus influenzae
hydantoin
3.5.1.88
0.001
-
IC50 against Escherichia coli peptide deformylase: 0.001 mM
Haemophilus influenzae
thyropropic acid derivatives
3.5.1.88
0.00104
-
IC50 against Escherichia coli peptide deformylase: 0.00104 mM
Haemophilus influenzae
benzothiazolylidene hydroxamic acid derivatives
3.5.1.88
0.00166
-
IC50 against Escherichia coli peptide deformylase: 0.00166 mM
Haemophilus influenzae
2-thioxo-4-thiazolidinone N-hexanoic acid
3.5.1.88
0.0022
-
IC50 against Escherichia coli peptide deformylase: 0.0022 mM
Haemophilus influenzae
N-hydroxy urea
3.5.1.88
0.0025
-
IC50 against Escherichia coli peptide deformylase: 0.0025 mM, designed based on the best substrate identified
Haemophilus influenzae
thiol peptide
3.5.1.88
0.0034
-
IC50 against Escherichia coli peptide deformylase: 0.0034 mM
Haemophilus influenzae
isoxazole-3-hydroxamic acid derivatives
3.5.1.88
0.01
-
IC50 against Escherichia coli peptide deformylase: 0.01 mM
Haemophilus influenzae
aldehyde peptide
3.5.1.88
0.2
-
IC50 against Escherichia coli peptide deformylase: 0.2 mM
Haemophilus influenzae
N-substituted methionine hydrazide
Application (protein specific)
EC Number
Application
Commentary
Organism
3.5.1.88
medicine
target for the development of new antibacterial drugs
Haemophilus influenzae
IC50 Value (protein specific)
EC Number
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
3.5.1.88
0.0000003
-
IC50 against Escherichia coli peptide deformylase: 0.0000003 mM
Haemophilus influenzae
actinonin
3.5.1.88
0.000003
-
IC50 against Escherichia coli peptide deformylase: 0.000003 mM
Haemophilus influenzae
N-alkyl urea hydroxamate
3.5.1.88
0.000004
0.00001
IC50 against Escherichia coli peptide deformylase: 0.000004-0.000010 mM
Haemophilus influenzae
alkyl-succinate-proline hydroxamate
3.5.1.88
0.000005
-
IC50: 0.000005 mM
Haemophilus influenzae
benzothiazinone derivatives
3.5.1.88
0.000016
-
IC50 against Escherichia coli peptide deformylase: 0.000016 mM
Haemophilus influenzae
beta-sulfonylhydroxamic acid
3.5.1.88
0.000019
-
IC50 against Escherichia coli peptide deformylase: 0.000019 mM, thiol chelating group combined with the best substrate motif
Haemophilus influenzae
thio peptide
3.5.1.88
0.00003
-
IC50 against Escherichia coli peptide deformylase: 0.000030 mM
Haemophilus influenzae
pseudopeptide metabolites
3.5.1.88
0.00012
-
IC50 against Escherichia coli peptide deformylase: 0.00012 mM
Haemophilus influenzae
quinazoline hydroxamic acid
3.5.1.88
0.0002
-
IC50 against Escherichia coli peptide deformylase: 0.0002 mM
Haemophilus influenzae
hydantoin
3.5.1.88
0.001
-
IC50 against Escherichia coli peptide deformylase: 0.001 mM
Haemophilus influenzae
thyropropic acid derivatives
3.5.1.88
0.00104
-
IC50 against Escherichia coli peptide deformylase: 0.00104 mM
Haemophilus influenzae
benzothiazolylidene hydroxamic acid derivatives
3.5.1.88
0.00166
-
IC50 against Escherichia coli peptide deformylase: 0.00166 mM
Haemophilus influenzae
2-thioxo-4-thiazolidinone N-hexanoic acid
3.5.1.88
0.0022
-
IC50 against Escherichia coli peptide deformylase: 0.0022 mM
Haemophilus influenzae
N-hydroxy urea
3.5.1.88
0.0025
-
IC50 against Escherichia coli peptide deformylase: 0.0025 mM, designed based on the best substrate identified
Haemophilus influenzae
thiol peptide
3.5.1.88
0.0034
-
IC50 against Escherichia coli peptide deformylase: 0.0034 mM
Haemophilus influenzae
isoxazole-3-hydroxamic acid derivatives
3.5.1.88
0.01
-
IC50 against Escherichia coli peptide deformylase: 0.01 mM
Haemophilus influenzae
aldehyde peptide
3.5.1.88
0.2
-
IC50 against Escherichia coli peptide deformylase: 0.2 mM
Haemophilus influenzae
N-substituted methionine hydrazide
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
3.5.1.88
2-oxo-pyrrolidine with chelators
-
Haemophilus influenzae
3.5.1.88
2-thioxo-4-thiazolidinone N-hexanoic acid
IC50 against Escherichia coli peptide deformylase: 0.00166 mM
Haemophilus influenzae
3.5.1.88
actinonin
IC50 against Escherichia coli peptide deformylase: 0.0000003 mM
Haemophilus influenzae
3.5.1.88
aldehyde peptide
IC50 against Escherichia coli peptide deformylase: 0.01 mM
Haemophilus influenzae
3.5.1.88
alkyl-succinate-proline hydroxamate
IC50 against Escherichia coli peptide deformylase: 0.000004-0.000010 mM
Haemophilus influenzae
3.5.1.88
benzimidazole N-formyl hydroxylamine
-
Haemophilus influenzae
3.5.1.88
benzothiazinone derivatives
IC50: 0.000005 mM
Haemophilus influenzae
3.5.1.88
benzothiazolylidene hydroxamic acid derivatives
IC50 against Escherichia coli peptide deformylase: 0.00104 mM
Haemophilus influenzae
3.5.1.88
beta-sulfonylhydroxamic acid
IC50 against Escherichia coli peptide deformylase: 0.000016 mM
Haemophilus influenzae
3.5.1.88
carbamate N-formyl hydroxylamine
-
Haemophilus influenzae
3.5.1.88
heteroarylaryl(P2'/P3')N-formyl hydroxylamine
-
Haemophilus influenzae
3.5.1.88
hydantoin
IC50 against Escherichia coli peptide deformylase: 0.0002 mM
Haemophilus influenzae
3.5.1.88
hydrazide N-formyl hydroxylamine
-
Haemophilus influenzae
3.5.1.88
isoxazole-3-hydroxamic acid derivatives
IC50 against Escherichia coli peptide deformylase: 0.0034 mM
Haemophilus influenzae
3.5.1.88
N-alkyl urea hydroxamate
IC50 against Escherichia coli peptide deformylase: 0.000003 mM
Haemophilus influenzae
3.5.1.88
N-hydroxy urea
IC50 against Escherichia coli peptide deformylase: 0.0022 mM
Haemophilus influenzae
3.5.1.88
N-hydroxy-2-(substituted phenyl) acetamide
-
Haemophilus influenzae
3.5.1.88
N-hydroxy-N-(3-hydrazino-3-oxopropyl)formamide
-
Haemophilus influenzae
3.5.1.88
N-substituted methionine hydrazide
IC50 against Escherichia coli peptide deformylase: 0.2 mM
Haemophilus influenzae
3.5.1.88
N-sulfonyl-L-Val-L-Leu-hydroxamate
-
Haemophilus influenzae
3.5.1.88
pseudopeptide metabolites
IC50 against Escherichia coli peptide deformylase: 0.000030 mM
Haemophilus influenzae
3.5.1.88
pyrrolidine bicyclic(P2'/P3')compounds
-
Haemophilus influenzae
3.5.1.88
quinazoline hydroxamic acid
IC50 against Escherichia coli peptide deformylase: 0.00012 mM
Haemophilus influenzae
3.5.1.88
thio peptide
IC50 against Escherichia coli peptide deformylase: 0.000019 mM, thiol chelating group combined with the best substrate motif
Haemophilus influenzae
3.5.1.88
thiol peptide
IC50 against Escherichia coli peptide deformylase: 0.0025 mM, designed based on the best substrate identified
Haemophilus influenzae
3.5.1.88
thyropropic acid derivatives
IC50 against Escherichia coli peptide deformylase: 0.001 mM
Haemophilus influenzae
3.5.1.88
urea analogs(P2'/P3')of N-formyl hydroxylamine
-
Haemophilus influenzae
Metals/Ions (protein specific)
EC Number
Metals/Ions
Commentary
Organism
Structure
3.5.1.88
Fe2+
-
Haemophilus influenzae
3.5.1.88
Ni2+
-
Haemophilus influenzae
3.5.1.88
Zn2+
-
Haemophilus influenzae
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.5.1.88
formyl-L-methionyl peptide + H2O
Haemophilus influenzae
-
formate + methionyl peptide
-
-
?
Oxidation Stability (protein specific)
EC Number
Oxidation Stability
Organism
3.5.1.88
ferrous ion in peptide deformylase is very unstable and is quickly and irreversibly oxidized to the ferric ion under laboratory conditions, resulting in an inactive enzyme.
Haemophilus influenzae
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.5.1.88
formyl-L-methionyl peptide + H2O
-
673200
Haemophilus influenzae
formate + methionyl peptide
-
-
-
?