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Literature summary for 3.4.15.1 extracted from

  • Watermeyer, J.M.; Kroeger, W.L.; O'Neill, H.G.; Sewell, B.T.; Sturrock, E.D.
    Probing the basis of domain-dependent inhibition using novel ketone inhibitors of angiotensin-converting enzyme (2008), Biochemistry, 47, 5942-5950.
    View publication on PubMed
Search for more literature for 3.4.15.1

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Chinese hamster ovary cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging drop vapour diffusion method, in 10 mM sodium acetate (pH 4.7), 15% PEG 4000, and 0.01 mM ZnSO4, at 16°C Homo sapiens

Protein Variants

Protein Variants Comment Organism
D453E the mutation does not contribute individually to C domain-selective inhibitor binding Homo sapiens
E403R the mutation does not contribute individually to C domain-selective inhibitor binding Homo sapiens
F391Y the F391Y mutation in the S2 pocket causes an 8fold decrease in inhibitor affinity relative to the wild type C domain Homo sapiens
S516N the S516N substitution results in a inhibitor binding affinity comparable to that of the wild type C domain Homo sapiens
T282S the mutation does not contribute individually to C domain-selective inhibitor binding Homo sapiens
V379/V380T the mutation displays small decrease in affinity for inhibitor (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-phenylalanine Homo sapiens
V379S the mutation does not contribute individually to C domain-selective inhibitor binding Homo sapiens
V380T the mutation displays small decrease in affinity for inhibitor (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-phenylalanine Homo sapiens
V518T the mutation shows the greatest decrease in affinity for inhibitor (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-phenylalanine the inhibitor has a 30fold higher affinity for the C domain than for the N domain of ACE Homo sapiens
(5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan the inhibitor shows strong C domain selectivity, having almost 1300-fold greater affinity for the C domain than for the N domain of ACE Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ contains zinc Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
angiotensin I + H2O Homo sapiens
-
 angiotensin II + L-His-L-Leu
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P12821
-
-

Purification (Commentary)

Purification (Comment) Organism
Sepharose-lisinopril affinity chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
testis
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
angiotensin I + H2O
-
 Homo sapiens angiotensin II + L-His-L-Leu
-
 ?
hippuryl-L-His-L-Leu + H2O
-
 Homo sapiens hippuric acid + L-His-L-Leu
-
 ?
Z-Phe-His-Leu + H2O
-
 Homo sapiens Z-Phe + His-Leu
-
 ?

Synonyms

Synonyms Comment Organism
ACE
-
 Homo sapiens
angiotensin-converting enzyme
-
 Homo sapiens
DCP
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000064
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan mutant enzyme V379S, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.00024
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan mutant enzyme E304R, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.000497
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan mutant enzyme S516N, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.000618
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan mutant enzyme D543E, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.000679
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan wild type enzyme, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.00081
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-phenylalanine mutant enzyme V379S, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.00083
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-phenylalanine wild type enzyme, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.00087
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan mutant enzyme V379S/V380T, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.00087
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan mutant enzyme V380T, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.00092
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan mutant enzyme T282S, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.0019
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-phenylalanine mutant enzyme V380T, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.00233
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan mutant enzyme E376D, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.0024
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-phenylalanine mutant enzyme E376D, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.0039
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-phenylalanine mutant enzyme F391Y, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.00475
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan mutant enzyme F391Y, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.00974
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan mutant enzyme V518T, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens
0.0181
-
 (5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-phenylalanine mutant enzyme V518T, in 50 mM HEPES buffer (pH 6.8) containing 200 mM NaCl, and 0.01 mM ZnCl2, at 25°C Homo sapiens