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Literature summary for 3.4.22.38 extracted from

  • McGrath, M.E.; Sprengeler, P.A.; Hill, C.M.; Martichonok, V.; Cheung, H.; Somoza, J.R.; Palmer, J.T.; Janc, J.W.
    Peptide ketobenzoxazole inhibitors bound to cathepsin K (2003), Biochemistry, 42, 15018-15028.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
crysallized from 20% MPD, 0.1 M Tris, pH 7 and 0.1 M MES, pH 6, crystals were flash frozen in a nitrogen stream after increasing the MPD concentration to aproximately 30% Oryctolagus cuniculus
hanging drop vapour diffusion method Homo sapiens

Protein Variants

Protein Variants Comment Organism
Y61D/V157L corresponding to the amino acid at that position in human enzyme, yields an enzyme with kinetic constants and inhibitor specificity profiles equivalent to human ortholog Oryctolagus cuniculus

Inhibitors

Inhibitors Comment Organism Structure
(S,S)-piperidine-4-carboxylic acid [1-[1-(benzoxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
Homo sapiens
(S,S)-piperidine-4-carboxylic acid [1-[1-(benzoxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
Oryctolagus cuniculus
piperidine-4-carboxylic acid [3-methyl-1[1-(1-oxa-3-aza-cyclopenta[a]naphthalene-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
Homo sapiens
piperidine-4-carboxylic acid [3-methyl-1[1-(1-oxa-3-aza-cyclopenta[a]naphthalene-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
Oryctolagus cuniculus
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
Homo sapiens
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
Oryctolagus cuniculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.019
-
CBZ-Phe-Arg-4-methylcoumarin 7-amide
-
Oryctolagus cuniculus
0.036
-
CBZ-Phe-Arg-4-methylcoumarin 7-amide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Oryctolagus cuniculus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens
-
Oryctolagus cuniculus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
CBZ-Phe-Arg-4-methylcoumarin 7-amide + H2O
-
Homo sapiens CBZ-Phe-Arg + 7-amino-4-methylcoumarin
-
?
CBZ-Phe-Arg-4-methylcoumarin 7-amide + H2O
-
Oryctolagus cuniculus CBZ-Phe-Arg + 7-amino-4-methylcoumarin
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate 21-24°C, pH 5.5 Homo sapiens
0.000002
-
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate 21-24°C, pH 5.5 Oryctolagus cuniculus