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Literature summary for 3.4.22.38 extracted from

  • Robichaud, J.; Oballa, R.; Prasit, P.; Falgueyret, J.P.; Percival, M.D.; Wesolowski, G.; Rodan, S.B.; Kimmel, D.; Johnson, C.; Bryant, C.; Venkatraman, S.; Setti, E.; Mendonca, R.; Palmer, J.T.
    A novel class of nonpeptidic biaryl inhibitors of human cathepsin K (2003), J. Med. Chem., 46, 3709-3727.
    View publication on PubMed
Search for more literature for 3.4.22.38

Cloned(Commentary)

Cloned (Comment) Organism
expression in Pichia pastoris Homo sapiens
expression in Pichia pastoris Oryctolagus cuniculus

Protein Variants

Protein Variants Comment Organism
S49A removing of a N-glycosylation site Homo sapiens
S49A removing of a N-glycosylation site Oryctolagus cuniculus
V157L humanization of rabbit enzyme Oryctolagus cuniculus
Y61D humanization of rabbit enzyme Oryctolagus cuniculus

Inhibitors

Inhibitors Comment Organism Structure
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide IC 50: 3 nM, reversible inhibition Homo sapiens
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
-
 Oryctolagus cuniculus

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.
Z-Leu-Arg-4-methylcoumarin 7-amide + H2O
-
 Homo sapiens Z-Leu-Arg + 7-amino-4-methylcoumarin
-
 ?
Z-Leu-Arg-4-methylcoumarin 7-amide + H2O
-
 Oryctolagus cuniculus Z-Leu-Arg + 7-amino-4-methylcoumarin
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000003
-
 IC 50: 3 nM, reversible inhibition Homo sapiens (2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide