Application | Comment | Organism |
---|---|---|
drug development | important drug target because of its role in the regulation of blood pressure via the renin-angiotensin-aldosterone system | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
purified recombinant mutant tACE-G13 in complex with inhibitor lisW-S, microseeding, 1.45 mg/ml tACE-G13 with 0.250 mM lisW-S over precipitant solution comprising 15% w/v PEG 4000, 0.010 mM ZnSO4, and 10 mM sodium acetate, pH 4.7, 2 weeks, X-ray diffraction structure determination and analysis at 2.3 A resolution, modelling | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D377Q | site-directed mutagenesis, altered inhibition kinetics with inhibitor lisW-S compared to the wild-type enzyme | Homo sapiens |
D453E | site-directed mutagenesis, altered inhibition kinetics with inhibitor lisW-S compared to the wild-type enzyme | Homo sapiens |
E162D | site-directed mutagenesis, altered inhibition kinetics with inhibitor lisW-S compared to the wild-type enzyme | Homo sapiens |
E376D | site-directed mutagenesis, altered inhibition kinetics with inhibitor lisW-S compared to the wild-type enzyme | Homo sapiens |
F391Y | site-directed mutagenesis, altered inhibition kinetics with inhibitor lisW-S compared to the wild-type enzyme | Homo sapiens |
additional information | construction of a minimally glycosylated tACE mutant, tACE-G13, truncated after Ser625 and lacking 36 O-glycosylated N-terminal residues as well as all but two N-glycosylation sites. Mutation of C-domain-specific active-site residues to their N-domain equivalents | Homo sapiens |
T282S | site-directed mutagenesis, altered inhibition kinetics with inhibitor lisW-S compared to the wild-type enzyme | Homo sapiens |
V379S | site-directed mutagenesis, altered inhibition kinetics with inhibitor lisW-S compared to the wild-type enzyme | Homo sapiens |
V380T | site-directed mutagenesis, altered inhibition kinetics with inhibitor lisW-S compared to the wild-type enzyme | Homo sapiens |
V518T | site-directed mutagenesis, altered inhibition kinetics with inhibitor lisW-S compared to the wild-type enzyme | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(5S)-5-[(N-benzoyl)-amino]-4-oxo-6-phenyl-hexanoyl-L-phenylalanine | phosphinic peptide inhibitor kAF | Homo sapiens | |
(5S)-5-[(N-benzoyl)amino]-4-oxo-6-phenylhexanoyl-L-tryptophan | phosphinic peptide inhibitor kAW | Homo sapiens | |
lisinopril | the compound shows a 4fold domain-selectivity for the C-domain compared to the N-domain. Active site binding structure, overview | Homo sapiens | |
lisW-S | a C-domain-selective derivative of the drug lisinopril. The compound shows a 258fold domain-selectivity for the C-domain compared to the N-domain, that is largely due to the co-operative effect of C-domain-specific residues in the S2' subsite. Interactions in the active site: comparison between N- and C-domain residues, overview | Homo sapiens | |
RXPA380 | - |
Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Zn2+ | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P12821 | - |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
glycoprotein | - |
Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
testis | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | ACE comprises two homologous domains, that differ in their substrate preferences, overview | Homo sapiens | ? | - |
? | |
o-aminobenzoyl-Phe-Arg-Lys(2,4-dinitrophenyl)-Pro-hydroxide + H2O | - |
Homo sapiens | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
More | ACE comprises two homologous domains, that differ in their substrate preferences, overview. Has a similar binding mode like its parent compound lisinopril, but the P2' tryptophan moiety takes a different conformation to that seen in other inhibitors having a tryptophan residue in this position | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
ACE | - |
Homo sapiens |
angiotensin-converting enzyme | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
6.8 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics of point exchange mutants with lisinopril and lisW-S, the mutants show highly decreased Ki for inhibitor lisW-S with their N-domain, overview | Homo sapiens | |
0.0000012 | - |
lisinopril | pH 6.8, 25°C, recombinant testis ACE C-domain | Homo sapiens | |
0.0000048 | - |
lisinopril | pH 6.8, 25°C, recombinant testis ACE N-domain | Homo sapiens | |
0.0000066 | - |
lisW-S | pH 6.8, 25°C, recombinant testis ACE C-domain | Homo sapiens | |
0.0017 | - |
lisW-S | pH 6.8, 25°C, recombinant testis ACE N-domain | Homo sapiens |