EC Number | Application | Comment | Organism |
---|---|---|---|
3.4.21.46 | drug development | the enzyme's exosite is a target for design of specific inhibitors for inhibition of the pathway complement activation in advanced dry age-related macular degeneration | Macaca fascicularis |
3.4.21.46 | drug development | the enzyme's exosite is a target for design of specific inhibitors for inhibition of the pathway complement activation in advanced dry age-related macular degeneration | Homo sapiens |
EC Number | Crystallization (Comment) | Organism |
---|---|---|
3.4.21.46 | purified enzyme in complex with anti-factor D Fab fragment, sitting drop vapor diffusion method, 20 mg/ml protein in 20 mM HEPES, pH 7.2, and 200 mM NaCl, is mixed with an equal volume of crystallization buffer containing 0.1 M MES, pH 6.5, 25% PEG monomethyl ether 550, 0.01 M zinc sulfate, and 3% 6-aminohexanoic acid, 1 day, 19°C, X-ray diffraction structure determination and analysis at 2.3 A resolution | Macaca fascicularis |
3.4.21.46 | purified enzyme in complex with anti-factor D Fab fragment, sitting drop vapor diffusion method, 30 mg/ml protein in 20 mM HEPES, pH 7.2, and 200 mM NaCl, is mixed with an equal volume of crystallization buffer containing 0.1 M Tris-HCl, pH 8.5, 0.2 M ammonium phosphate, 50% 2-methyl-2,4-pentanediol, and 0.01 M hexamine cobalt(III) chloride, 6 days, 4°C, X-ray diffraction structure determination and analysis at 2.4 A resolution | Homo sapiens |
EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
3.4.21.46 | anti-factor D Fab fragment | an Escherichia coli-expressed, humanized Fab fragment, derived from monoclonal antibody 166-32, and designed as specific enzyme inhibitor targeting the exosite. Anti-factor D Fab fragment prevents factor D-mediated proteolytic activation of its macromolecular substrate C3bB, but not proteolysis of a small synthetic substrate, indicating that the inhibitor does not block access of the substrate to the catalytic site, binding structure and inhibitory mechanism, overview. The structures show that the AFD-binding site includes surface loops of the enzyme that form part of the enzyme's exosite. Anti-factor D Fab fragment inhibits the enzyme proteolytic function by interfering with macromolecular substrate access rather than by inhibiting the enzyme catalysis | Homo sapiens | |
3.4.21.46 | anti-factor D Fab fragment | an Escherichia coli-expressed, humanized Fab fragment, derived from monoclonal antibody 166-32, and designed as specific enzyme inhibitor targeting the exosite. Anti-factor D Fab fragment prevents factor D-mediated proteolytic activation of its macromolecular substrate C3bB, but not proteolysis of a small synthetic substrate, indicating that the inhibitor does not block access of the substrate to the catalytic site, binding structure and inhibitory mechanism, overview. The structures show that the AFD-binding site includes surface loops of the enzyme that form part of the enzyme's exosite. Anti-factor D Fab fragment inhibits the enzyme proteolytic function by interfering with macromolecular substrate access rather than by inhibiting the enzyme catalysis | Macaca fascicularis |
EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
3.4.21.46 | complement component C3bB + H2O | Macaca fascicularis | - |
? | - |
? | |
3.4.21.46 | complement component C3bB + H2O | Homo sapiens | - |
? | - |
? |
EC Number | Organism | UniProt | Comment | Textmining |
---|---|---|---|---|
3.4.21.46 | Homo sapiens | P00746 | - |
- |
3.4.21.46 | Macaca fascicularis | - |
- |
- |
EC Number | Purification (Comment) | Organism |
---|---|---|
3.4.21.46 | enzyme and inhibitor by gel filtration | Homo sapiens |
EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|---|
3.4.21.46 | complement component C3bB + H2O | - |
Macaca fascicularis | ? | - |
? | |
3.4.21.46 | complement component C3bB + H2O | - |
Homo sapiens | ? | - |
? |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
3.4.21.46 | factor D | - |
Macaca fascicularis |
3.4.21.46 | factor D | - |
Homo sapiens |
EC Number | General Information | Comment | Organism |
---|---|---|---|
3.4.21.46 | physiological function | targeting of the enzyme's exosite causes inhibition of the pathway complement activation | Macaca fascicularis |
3.4.21.46 | physiological function | targeting of the enzyme's exosite causes inhibition of the pathway complement activation | Homo sapiens |