Literature summary for 3.4.19.6 extracted from

  • Kelly, J.A.; Slator, G.R.; Tipton, K.F.; Williams, C.H.; Bauer, K.
    Kinetic investigation of the specificity of porcine brain thyrotropin-releasing hormone-degrading ectoenzyme for thyrotropin-releasing hormone-like peptides (2000), J. Biol. Chem., 275, 16746-16751.
    View publication on PubMed

Application

Application Comment Organism
medicine inhibitors of the enzyme may be used to enhance the therapeutic actions of TRH and to investigate the functions of thyrotropin-releasing hormone and pyroglutamyl-peptidase II Sus scrofa

Inhibitors

Inhibitors Comment Organism Structure
L-pyroglutamyl-Asn-Pro-NH2 inhibition is fully reversible Sus scrofa
pyroglutamyl-Asn-Pro-7-amido-4-methyl coumarin
-
Sus scrofa
pyroglutamyl-Asn-Pro-NH2
-
Sus scrofa
pyroglutamyl-Gln-Pro-NH2
-
Sus scrofa
pyroglutamyl-Gly-Pro-NH2 inhibition is fully reversible Sus scrofa
pyroglutamyl-homoprolyl-Pro-NH2
-
Sus scrofa
pyroglutamyl-L-alpha-phenylglycyl-Pro-NH2
-
Sus scrofa
pyroglutamyl-Trp-Pro-NH2
-
Sus scrofa

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.015
-
L-pyroglutamyl-L-Tyr-L-Pro-NH2 pH 7.5, 37°C Sus scrofa
0.034
-
pyroglutamyl-thienylalanyl-Pro-NH2 pH 7.5, 37°C Sus scrofa
0.055
-
pyroglutamyl-Phe-Pro-NH2 pH 7.5, 37°C Sus scrofa
0.035
-
pyroglutamyl-His-Pro-NH2 pH 7.5, 37°C Sus scrofa
0.0035
-
pyroglutamyl-His-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Sus scrofa
0.311
-
pyroglutamyl-His-Pro-OH pH 7.5, 37°C Sus scrofa

Organism

Organism UniProt Comment Textmining
Sus scrofa
-
-
-

Purification (Commentary)

Purification (Comment) Organism
enzyme from brain Sus scrofa

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Sus scrofa
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information moderately bulky, uncharged P1' residues preferentially bind to the enzyme Sus scrofa ?
-
?
pyroglutamyl-Phe-Pro-NH2 + H2O
-
Sus scrofa pyroglutamate + Phe-Pro-NH2
-
?
thyroliberin + H2O
-
Sus scrofa pyroglutamic acid + His-Pro-NH2
-
?
pyroglutamyl-His-Pro-OH + H2O
-
Sus scrofa pyroglutamate + His-Pro-OH
-
?
pyroglutamyl-His-Pro-NH2 + H2O
-
Sus scrofa pyroglutamate + His-Pro-NH2
-
?
pyroglutamyl-thienylalanyl-Pro-NH2 + H2O
-
Sus scrofa pyroglutamate + thienylalanyl-Pro-NH2
-
?
pyroglutamyl-Phe-Pro-OH + H2O
-
Sus scrofa pyroglutamate + Phe-Pro-OH
-
?
pyroglutamyl-Tyr-Pro-OH + H2O
-
Sus scrofa pyroglutamate + Tyr-Pro-OH
-
?
pyroglutamyl-His-Pro-7-amido-4-methylcoumarin + H2O
-
Sus scrofa pyroglutamate + His-Pro-7-amido-4-methylcoumarin
-
?
L-pyroglutamyl-L-Tyr-L-Pro-NH2 + H2O
-
Sus scrofa L-pyroglutamate + L-Tyr-L-Pro-NH2
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0175
-
pyroglutamyl-Asn-Pro-NH2 pH 7.5, 37°C, hydrolysis of pyroglutamyl-His-Pro-7-amido-4-methylcoumarin Sus scrofa
0.5
-
pyroglutamyl-homoprolyl-Pro-NH2 pH 7.5, 37°C, hydrolysis of pyroglutamyl-His-Pro-7-amido-4-methylcoumarin Sus scrofa
0.069
-
pyroglutamyl-Gln-Pro-NH2 pH 7.5, 37°C, hydrolysis of pyroglutamyl-His-Pro-7-amido-4-methylcoumarin Sus scrofa
0.00097
-
pyroglutamyl-Asn-Pro-7-amido-4-methyl coumarin pH 7.5, 37°C, hydrolysis of pyroglutamyl-His-Pro-7-amido-4-methylcoumarin Sus scrofa
0.232
-
pyroglutamyl-Trp-Pro-NH2 pH 7.5, 37°C, hydrolysis of pyroglutamyl-His-Pro-7-amido-4-methylcoumarin Sus scrofa
0.356
-
pyroglutamyl-L-alpha-phenylglycyl-Pro-NH2 pH 7.5, 37°C, hydrolysis of pyroglutamyl-His-Pro-7-amido-4-methylcoumarin Sus scrofa