Cloned (Comment) | Organism |
---|---|
expressed in Chinese hamster ovary cells | Homo sapiens |
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 | 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 | 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 | Comment | Organism | Structure |
---|---|---|---|
Zn2+ | contains zinc | Homo sapiens |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P12821 | - |
- |
Purification (Comment) | Organism |
---|---|
Sepharose-lisinopril affinity chromatography | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
testis | - |
Homo sapiens | - |
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 | Comment | Organism |
---|---|---|
ACE | - |
Homo sapiens |
angiotensin-converting enzyme | - |
Homo sapiens |
DCP | - |
Homo sapiens |
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 |