Cloned (Comment) | Organism |
---|---|
expression of a cDNA encoding the fragment Gly106-Gly263 of the enzyme F171D mutant in Escherichia coli strain BL21 | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
purified MMP-12 bound to hydroxamic acid, hanging drop vapour diffusion method, 20°C, from protein solution containing 10 mg/ml protein in 0.1 M Tris-HCl, pH 8.0, 30% PEG 6000, 200 mM hydroxamic acid, and 1.0 M LiCl, a few days, X-ray diffraction structure determination and analysis at 1.3 A resolution | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(1S,5S,7R)-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-3,7-dicarboxylic acid 7-[(biphenyl-4-ylmethyl)-amide] 3-hydroxyamide | - |
Homo sapiens | |
(1S,5S,7R)-3-biphenyl-4-ylmethyl-2-oxo-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-7-carboxylic acid | - |
Homo sapiens | |
(1S,5S,7R)-3-biphenyl-4-ylmethyl-2-oxo-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-7-carboxylic acid hydroxyamide | - |
Homo sapiens | |
(1S,5S,7R)-3-biphenyl-4-ylmethyl-3-aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic acid | - |
Homo sapiens | |
(1S,5S,7R)-3-biphenyl-4-ylmethyl-3-aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic acid hydroxyamide | - |
Homo sapiens | |
additional information | inhibitor design and synthesis based on a 3-aza-6,8-dioxa-bicyclo[3.2.1]octane scaffold, library construction and screening, determination of affinity for the catalytic domain of MMP-12 by NMR, overview | Homo sapiens | |
N-isobutyl-N-[4-methoxyphenylsulfonyl] glycyl hydroxamic acid | - |
Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Ca2+ | - |
Homo sapiens | |
Zn2+ | zinc metalloprotease | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
recombinant F171D mutant fragment Gly106-Gly263 from Escherichia coli strain BL21 by gel filtration and anion exchange chromatography | Homo sapiens |
Renatured (Comment) | Organism |
---|---|
recombinant fragment of mutant F171D from Escherichia coli inclusion bodies by solubilization in 20 mM Tris-HCl and 8 M urea at pH 8.0, refolding by multi-step dialysis, overview | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 + H2O | - |
Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Human macrophage metalloelastase | - |
Homo sapiens |
macrophage metalloelastase | - |
Homo sapiens |
MMP-12 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.954 | - |
pH 7.0, 25°C, recombinant enzyme | Homo sapiens | (1S,5S,7R)-3-biphenyl-4-ylmethyl-2-oxo-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-7-carboxylic acid | |
149 | - |
pH 7.0, 25°C, recombinant enzyme | Homo sapiens | (1S,5S,7R)-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-3,7-dicarboxylic acid 7-[(biphenyl-4-ylmethyl)-amide] 3-hydroxyamide | |
399 | - |
pH 7.0, 25°C, recombinant enzyme | Homo sapiens | (1S,5S,7R)-3-biphenyl-4-ylmethyl-3-aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic acid hydroxyamide | |
425 | - |
pH 7.0, 25°C, recombinant enzyme | Homo sapiens | (1S,5S,7R)-3-biphenyl-4-ylmethyl-2-oxo-3-aza-6,8-dioxa-bicyclo[3.2.1]octane-7-carboxylic acid hydroxyamide | |
835 | - |
pH 7.0, 25°C, recombinant enzyme | Homo sapiens | (1S,5S,7R)-3-biphenyl-4-ylmethyl-3-aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic acid |