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Literature summary for 3.4.24.15 extracted from

  • Steer, D.; Lew, R.; Perlmutter, P.; Smith, A.I.; Aguilar, M.I.
    Inhibitors of metalloendopeptidase EC 3.4.24.15 and EC 3.4.24.16 stabilized against proteolysis by the incorporation of beta-amino acids (2002), Biochemistry, 41, 10819-10826.
    View publication on PubMed
Search for more literature for 3.4.24.15

Inhibitors

Inhibitors Comment Organism Structure
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-((3S)-pyrrolidine-3-carboxyl)-Phe-(3-aminopropanoic acid) IC50: 0.0063 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-((3S)-pyrrolidine-3-carboxyl)-Tyr-(3-aminopropanoic acid) IC50: 0.0069 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-amino-2-methylpropanoyl)-((3R)-3-amino-4-phenylbutanoyl)-(3-aminopropanoic acid) IC50: 0.0794 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-amino-2-methylpropanoyl)-((3S)-3-amino-4-phenylbutanoyl)-(3-aminopropanoic acid) IC50: 0.0631 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-amino-2-methylpropanoyl)-(2-aminomethyl-3-phenylpropionyl)-(3-aminopropanoic acid) IC50: 0.158 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-amino-2-methylpropanoyl)-Phe-(3-aminopropanoic acid) IC50: 0.0028 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-amino-2-methylpropanoyl)-Tyr-3-aminopropanoic acid IC50: 0.0063 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-aminopropanoyl)-Tyr-(3-aminopropanoic acid) IC50: 0.0056 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(piperidine-3-carboxyl)-Phe-(3-aminopropanoic acid) IC50: 0.01 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(piperidine-3-carboxyl)-Tyr-(3-aminopropanoic acid) IC50: 0.0056 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala-((3S)-3-amino-4-(4-hydroxyphenyl)butanoyl)-(3-aminopropanoic acid) IC50: 0.0251 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala-beta-2-Phe-(3-aminopropanoylic acid) IC50: 0.04 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala-Phe-(3-aminopropanoic acid) IC50: 0.0036 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala-Tyr-(3-aminopropanoic acid) IC50: 0.00012 mM, complete degradation by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala-Tyr-p-aminobenzoate IC50: 0.00006 mM, potent and specific inhibitor, unstable in vivo due to cleavage between the alanine and tyrosine residues by the enzyme nephrilysin. This cleavage generates a potent inhibitor of angiotensin converting enzyme, thereby limiting the use of the inhibitor for in vivo studies Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Pro-Phe-(3-aminopropanoic acid) IC50: 0.00079 mM, no cleavage by nephrilysin Rattus norvegicus
N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Pro-Tyr-(3-aminopropanoic acid) IC50: 0.00066 mM, no cleavage by nephrilysin Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
testis
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-D-Lys-(2,4-dinitrophenyl) + H2O
-
 Rattus norvegicus ?
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00006
-
 IC50: 0.00006 mM, potent and specific inhibitor, unstable in vivo due to cleavage between the alanine and tyrosine residues by the enzyme nephrilysin. This cleavage generates a potent inhibitor of angiotensin converting enzyme, thereby limiting the use of Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala-Tyr-p-aminobenzoate
0.00012
-
 IC50: 0.00012 mM, complete degradation by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala-Tyr-(3-aminopropanoic acid)
0.00066
-
 IC50: 0.00066 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Pro-Tyr-(3-aminopropanoic acid)
0.00079
-
 IC50: 0.00079 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Pro-Phe-(3-aminopropanoic acid)
0.0028
-
 IC50: 0.0028 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-amino-2-methylpropanoyl)-Phe-(3-aminopropanoic acid)
0.0036
-
 IC50: 0.0036 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala-Phe-(3-aminopropanoic acid)
0.0056
-
 IC50: 0.0056 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-aminopropanoyl)-Tyr-(3-aminopropanoic acid)
0.0056
-
 IC50: 0.0056 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(piperidine-3-carboxyl)-Tyr-(3-aminopropanoic acid)
0.0063
-
 IC50: 0.0063 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-amino-2-methylpropanoyl)-Tyr-3-aminopropanoic acid
0.0063
-
 IC50: 0.0063 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-((3S)-pyrrolidine-3-carboxyl)-Phe-(3-aminopropanoic acid)
0.0069
-
 IC50: 0.0069 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-((3S)-pyrrolidine-3-carboxyl)-Tyr-(3-aminopropanoic acid)
0.01
-
 IC50: 0.01 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(piperidine-3-carboxyl)-Phe-(3-aminopropanoic acid)
0.0251
-
 IC50: 0.0251 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala-((3S)-3-amino-4-(4-hydroxyphenyl)butanoyl)-(3-aminopropanoic acid)
0.04
-
 IC50: 0.04 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-Ala-beta-2-Phe-(3-aminopropanoylic acid)
0.0631
-
 IC50: 0.0631 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-amino-2-methylpropanoyl)-((3S)-3-amino-4-phenylbutanoyl)-(3-aminopropanoic acid)
0.0794
-
 IC50: 0.0794 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-amino-2-methylpropanoyl)-((3R)-3-amino-4-phenylbutanoyl)-(3-aminopropanoic acid)
0.158
-
 IC50: 0.158 mM, no cleavage by nephrilysin Rattus norvegicus N-[1-(R,S)-carboxy-3-phenylpropyl]-Ala-(3-amino-2-methylpropanoyl)-(2-aminomethyl-3-phenylpropionyl)-(3-aminopropanoic acid)