Literature summary for 3.5.1.88 extracted from

Jain, R.; Chen, D.; White, R.J.; Patel, D.V.; Yuan, Z.
Bacterial Peptide deformylase inhibitors: a new class of antibacterial agents (2005), Curr. Med. Chem., 12, 1607-1621.

Application

Application	Comment	Organism
medicine	target for the development of new antibacterial drugs	Haemophilus influenzae

Inhibitors

Inhibitors	Comment	Organism
2-oxo-pyrrolidine with chelators	-	Haemophilus influenzae
2-thioxo-4-thiazolidinone N-hexanoic acid	IC50 against Escherichia coli peptide deformylase: 0.00166 mM	Haemophilus influenzae
actinonin	IC50 against Escherichia coli peptide deformylase: 0.0000003 mM	Haemophilus influenzae
aldehyde peptide	IC50 against Escherichia coli peptide deformylase: 0.01 mM	Haemophilus influenzae
alkyl-succinate-proline hydroxamate	IC50 against Escherichia coli peptide deformylase: 0.000004-0.000010 mM	Haemophilus influenzae
benzimidazole N-formyl hydroxylamine	-	Haemophilus influenzae
benzothiazinone derivatives	IC50: 0.000005 mM	Haemophilus influenzae
benzothiazolylidene hydroxamic acid derivatives	IC50 against Escherichia coli peptide deformylase: 0.00104 mM	Haemophilus influenzae
beta-sulfonylhydroxamic acid	IC50 against Escherichia coli peptide deformylase: 0.000016 mM	Haemophilus influenzae
carbamate N-formyl hydroxylamine	-	Haemophilus influenzae
heteroarylaryl(P2'/P3')N-formyl hydroxylamine	-	Haemophilus influenzae
hydantoin	IC50 against Escherichia coli peptide deformylase: 0.0002 mM	Haemophilus influenzae
hydrazide N-formyl hydroxylamine	-	Haemophilus influenzae
isoxazole-3-hydroxamic acid derivatives	IC50 against Escherichia coli peptide deformylase: 0.0034 mM	Haemophilus influenzae
N-alkyl urea hydroxamate	IC50 against Escherichia coli peptide deformylase: 0.000003 mM	Haemophilus influenzae
N-hydroxy urea	IC50 against Escherichia coli peptide deformylase: 0.0022 mM	Haemophilus influenzae
N-hydroxy-2-(substituted phenyl) acetamide	-	Haemophilus influenzae
N-hydroxy-N-(3-hydrazino-3-oxopropyl)formamide	-	Haemophilus influenzae
N-substituted methionine hydrazide	IC50 against Escherichia coli peptide deformylase: 0.2 mM	Haemophilus influenzae
N-sulfonyl-L-Val-L-Leu-hydroxamate	-	Haemophilus influenzae
pseudopeptide metabolites	IC50 against Escherichia coli peptide deformylase: 0.000030 mM	Haemophilus influenzae
pyrrolidine bicyclic(P2'/P3')compounds	-	Haemophilus influenzae
quinazoline hydroxamic acid	IC50 against Escherichia coli peptide deformylase: 0.00012 mM	Haemophilus influenzae
thio peptide	IC50 against Escherichia coli peptide deformylase: 0.000019 mM, thiol chelating group combined with the best substrate motif	Haemophilus influenzae
thiol peptide	IC50 against Escherichia coli peptide deformylase: 0.0025 mM, designed based on the best substrate identified	Haemophilus influenzae
thyropropic acid derivatives	IC50 against Escherichia coli peptide deformylase: 0.001 mM	Haemophilus influenzae
urea analogs(P2'/P3')of N-formyl hydroxylamine	-	Haemophilus influenzae

Metals/Ions

Metals/Ions	Comment	Organism
Fe2+	-	Haemophilus influenzae
Ni2+	-	Haemophilus influenzae
Zn2+	-	Haemophilus influenzae

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
formyl-L-methionyl peptide + H2O	Haemophilus influenzae	-	formate + methionyl peptide	-	?

Organism

Organism	UniProt	Comment	Textmining
Haemophilus influenzae	-	-	-

Oxidation Stability

Oxidation Stability	Organism
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)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
formyl-L-methionyl peptide + H2O	-	Haemophilus influenzae	formate + methionyl peptide	-	?

Synonyms

Synonyms	Comment	Organism
PDF	-	Haemophilus influenzae
peptide deformylase	-	Haemophilus influenzae

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.0000003	-	IC50 against Escherichia coli peptide deformylase: 0.0000003 mM	Haemophilus influenzae	actinonin
0.000003	-	IC50 against Escherichia coli peptide deformylase: 0.000003 mM	Haemophilus influenzae	N-alkyl urea hydroxamate
0.000004	0.00001	IC50 against Escherichia coli peptide deformylase: 0.000004-0.000010 mM	Haemophilus influenzae	alkyl-succinate-proline hydroxamate
0.000005	-	IC50: 0.000005 mM	Haemophilus influenzae	benzothiazinone derivatives
0.000016	-	IC50 against Escherichia coli peptide deformylase: 0.000016 mM	Haemophilus influenzae	beta-sulfonylhydroxamic acid
0.000019	-	IC50 against Escherichia coli peptide deformylase: 0.000019 mM, thiol chelating group combined with the best substrate motif	Haemophilus influenzae	thio peptide
0.00003	-	IC50 against Escherichia coli peptide deformylase: 0.000030 mM	Haemophilus influenzae	pseudopeptide metabolites
0.00012	-	IC50 against Escherichia coli peptide deformylase: 0.00012 mM	Haemophilus influenzae	quinazoline hydroxamic acid
0.0002	-	IC50 against Escherichia coli peptide deformylase: 0.0002 mM	Haemophilus influenzae	hydantoin
0.001	-	IC50 against Escherichia coli peptide deformylase: 0.001 mM	Haemophilus influenzae	thyropropic acid derivatives
0.00104	-	IC50 against Escherichia coli peptide deformylase: 0.00104 mM	Haemophilus influenzae	benzothiazolylidene hydroxamic acid derivatives
0.00166	-	IC50 against Escherichia coli peptide deformylase: 0.00166 mM	Haemophilus influenzae	2-thioxo-4-thiazolidinone N-hexanoic acid
0.0022	-	IC50 against Escherichia coli peptide deformylase: 0.0022 mM	Haemophilus influenzae	N-hydroxy urea
0.0025	-	IC50 against Escherichia coli peptide deformylase: 0.0025 mM, designed based on the best substrate identified	Haemophilus influenzae	thiol peptide
0.0034	-	IC50 against Escherichia coli peptide deformylase: 0.0034 mM	Haemophilus influenzae	isoxazole-3-hydroxamic acid derivatives
0.01	-	IC50 against Escherichia coli peptide deformylase: 0.01 mM	Haemophilus influenzae	aldehyde peptide
0.2	-	IC50 against Escherichia coli peptide deformylase: 0.2 mM	Haemophilus influenzae	N-substituted methionine hydrazide