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Literature summary for 3.5.1.88 extracted from

  • Green, B.G.; Toney, J.H.; Kozarich, J.W.; Grant, S.K.
    Inhibition of bacterial peptide deformylase by biaryl acid analogs (2000), Arch. Biochem. Biophys., 375, 355-358.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Escherichia coli

Protein Variants

Protein Variants Comment Organism
additional information C-terminally histidine-tagged, PDF-H6, is well expressed and has identical physical and catalytic properties as the wild-type enzyme, N-terminally histidine-tagged enzyme shows drastically reduced catalytic activity Escherichia coli

General Stability

General Stability Organism
enhanced in vitro stability by binding of Zn2+ Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
2-butyl-5,7-dimethyl-3-[2''-(1H-tetrazol-5-ylmethyl)-[1,1',4',1'']terphenyl-4-yl]-3H-imidazo[4,5-b]pyridine belongs to a class of angiotensin II receptor antagonists, potent inhibitor, IC50: 0.0076 mM Escherichia coli
3-[5'-benzyl-2'-(1H-tetrazol-5-yl)-biphenyl-4-yl]-2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridine potent inhibitor, IC50: 0.0342 mM, the acidic moiety forms direct ionic interactions with active site metal cation Escherichia coli
5-chloro-2-propyl-3-[2''-(1H-tetrazol-5-ylmethyl)-[1,1',4',1'']terphenyl-4-yl]-3H-imidazo[4,5-b]pyridine belongs to a broad class of angiotensin II receptor antagonists, potent competitive inhibitor, IC50: 0.0039 mM, the acidic moiety forms direct ionic interactions with active site metal cation Escherichia coli
butyl {[4'-(2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridin-3-yl)-5-(2-methylbutan-2-yl)biphenyl-2-yl]sulfonyl}carbamate competitive inhibition, IC50: 0.015 mM, the acidic moiety forms direct ionic interactions with active site metal cation Escherichia coli

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
8.8
-
N-formyl-L-Met-Val
-
Escherichia coli

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ 10fold more active than Co2+-prepared enzyme Escherichia coli

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
N-formyl-L-methionine-polypeptide + H2O Escherichia coli the enzyme is involved in maturation of proteins by cleaving the N-formyl group from N-blocked methionine polypeptides formate + L-methionine-polypeptide
-
?

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
C-terminally truncated recombinant enzyme
-

Oxidation Stability

Oxidation Stability Organism
sensitive to intracellular reactive oxygen Escherichia coli

Purification (Commentary)

Purification (Comment) Organism
to homogeneity, recombinant C-terminal truncated enzyme, preliminary Zn2+-bound, 10fold more active than Co2+-bound enzyme Escherichia coli

Source Tissue

Source Tissue Comment Organism Textmining
cell culture
-
Escherichia coli
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-formyl-L-Met-Val + H2O
-
Escherichia coli formate + L-Met-Val
-
?
N-formyl-L-methionine-polypeptide + H2O the enzyme is involved in maturation of proteins by cleaving the N-formyl group from N-blocked methionine polypeptides Escherichia coli formate + L-methionine-polypeptide
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0012
-
3-[5'-benzyl-2'-(1H-tetrazol-5-yl)-biphenyl-4-yl]-2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridine
-
Escherichia coli
0.006
-
butyl {[4'-(2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridin-3-yl)-5-(2-methylbutan-2-yl)biphenyl-2-yl]sulfonyl}carbamate
-
Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0039
-
belongs to a broad class of angiotensin II receptor antagonists, potent competitive inhibitor, IC50: 0.0039 mM, the acidic moiety forms direct ionic interactions with active site metal cation Escherichia coli 5-chloro-2-propyl-3-[2''-(1H-tetrazol-5-ylmethyl)-[1,1',4',1'']terphenyl-4-yl]-3H-imidazo[4,5-b]pyridine
0.0076
-
belongs to a class of angiotensin II receptor antagonists, potent inhibitor, IC50: 0.0076 mM Escherichia coli 2-butyl-5,7-dimethyl-3-[2''-(1H-tetrazol-5-ylmethyl)-[1,1',4',1'']terphenyl-4-yl]-3H-imidazo[4,5-b]pyridine
0.015
-
competitive inhibition, IC50: 0.015 mM, the acidic moiety forms direct ionic interactions with active site metal cation Escherichia coli butyl {[4'-(2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridin-3-yl)-5-(2-methylbutan-2-yl)biphenyl-2-yl]sulfonyl}carbamate
0.0342
-
potent inhibitor, IC50: 0.0342 mM, the acidic moiety forms direct ionic interactions with active site metal cation Escherichia coli 3-[5'-benzyl-2'-(1H-tetrazol-5-yl)-biphenyl-4-yl]-2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridine