Application | Comment | Organism |
---|---|---|
medicine | enhancing cocaine metabolism by administration of cocaine esterase (CocE) is a promising treatment strategy for cocaine overdose and addiction, because CocE is the most efficient native enzyme for metabolizing the naturally occurring cocaine. A major obstacle to the clinical application of CocE is the thermoinstability of native CocE with a half-life of only a few min at physiological temperature. Computational-experimental effort yields a CocE variant with a 30fold increase in plasma half-life both in vitro and in vivo | Rhodococcus sp. |
Protein Variants | Comment | Organism |
---|---|---|
G173Q | kcat and Km-value for cocaine is similar to wild-type value, half-life is increased 7fold compared to wild-type enzyme | Rhodococcus sp. |
additional information | computational-experimental effort yields a CocE variant with a 30-fold increase in plasma half-life both in vitro and in vivo | Rhodococcus sp. |
T172R | kcat and Km-value for cocaine is similar to wild-type value, half-life is increased 7fold compared to wild-type enzyme | Rhodococcus sp. |
T172R/G173Q | kcat and Km-value for cocaine is similar to wild-type value, half-life is increased 30fold compared to wild-type enzyme | Rhodococcus sp. |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.015 | - |
cocaine | ph 7.4, 37°C, mutant enzyme G173Q | Rhodococcus sp. | |
0.021 | - |
cocaine | pH 7.4, 37°C, wild-type enzyme | Rhodococcus sp. | |
0.024 | - |
cocaine | ph 7.4, 37°C, mutant enzyme T172R | Rhodococcus sp. | |
0.024 | - |
cocaine | ph 7.4, 37°C, mutant enzyme T172R/G173Q | Rhodococcus sp. |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
cocaine + H2O | Rhodococcus sp. | CocE is the most efficient native enzyme for metabolizing the naturally occurring cocaine | ecgonine methyl ester + benzoate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rhodococcus sp. | Q9L9D7 | - |
- |
Purification (Comment) | Organism |
---|---|
- |
Rhodococcus sp. |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
cocaine + H2O | - |
Rhodococcus sp. | ecgonine methyl ester + benzoate | - |
? | |
cocaine + H2O | CocE is the most efficient native enzyme for metabolizing the naturally occurring cocaine | Rhodococcus sp. | ecgonine methyl ester + benzoate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
cocE | - |
Rhodococcus sp. |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Rhodococcus sp. |
Temperature Stability Minimum [°C] | Temperature Stability Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
half-life: 11 min (wild-type enzyme), 78 min (mutant enzyme T172R), 75 min (mutant enzyme G173Q), 305 min (mutant enzyme T172R/G173Q) | Rhodococcus sp. |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
2247 | - |
cocaine | ph 7.4, 37°C, mutant enzyme T172R/G173Q | Rhodococcus sp. | |
2323 | - |
cocaine | pH 7.4, 37°C, wild-type enzyme | Rhodococcus sp. | |
2384 | - |
cocaine | ph 7.4, 37°C, mutant enzyme G173Q | Rhodococcus sp. | |
2502 | - |
cocaine | ph 7.4, 37°C, mutant enzyme T172R | Rhodococcus sp. |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Rhodococcus sp. |