Application | Comment | Organism |
---|---|---|
medicine | the bleomycins (BLMs) are widely used in combination therapies for the treatment of various cancers. Dose-dependent and cumulative pulmonary toxicity is the major cause of BLM-associated morbidity, limiting the broad uses of BLMs as anticancer drugs. Opportunities to overcome bleomycin-induced pulmonary toxicity in chemotherapies, potentially by exploring BLM B2 as the preferred congener, engineering designer bleomycins with optimized activity for recombinant human bleomycin hydrolase (rhBLMH), or co-administrating rhBLMH directly into the lung as a potential protein therapeutic | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expression in Escherichia coli | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.19 | - |
bleomycin B2 | pH 7.5, 30°C | Homo sapiens | |
0.592 | - |
bleomycin A2 | pH 7.5, 30°C | Homo sapiens | |
0.72 | - |
6'-deoxy tallysomycin H1 | pH 7.5, 30°C | Homo sapiens | |
0.743 | - |
tallysomycin H1 | pH 7.5, 30°C | Homo sapiens | |
0.805 | - |
6'-deoxy bleomycin A2 | pH 7.5, 30°C | Homo sapiens | |
0.854 | - |
bleomycin Z | pH 7.5, 30°C | Homo sapiens | |
0.942 | - |
6'-deoxy bleomycin Z | pH 7.5, 30°C | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
bleomycin A2 + H2O | Homo sapiens | the enzyme hydrolyzes bleomycins into the biologically inactive deamido bleomycins | deamido bleomycin A2 + NH3 | - |
? | |
bleomycin B2 + H2O | Homo sapiens | the enzyme hydrolyzes bleomycins into the biologically inactive deamido bleomycins | deamido bleomycin B2 + NH3 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q13867 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
lung | poorly expressed in the lung | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
6'-deoxy bleomycin A2 + H2O | recombinant enzyme shows rapid and efficient hydrolysis of all bleomycins tested, exhibiting a superior catalytic efficiency for bleomycin B2 | Homo sapiens | 6'-deoxy deamido bleomycin A2 + NH3 | - |
? | |
6'-deoxy bleomycin Z + H2O | recombinant enzyme shows rapid and efficient hydrolysis of all bleomycins tested, exhibiting a superior catalytic efficiency for bleomycin B2 | Homo sapiens | 6'-deoxy deamido bleomycin Z + NH3 | - |
? | |
6'-deoxy tallysomycin H1 + H2O | - |
Homo sapiens | ? + NH3 | - |
? | |
bleomycin A2 + H2O | the enzyme hydrolyzes bleomycins into the biologically inactive deamido bleomycins | Homo sapiens | deamido bleomycin A2 + NH3 | - |
? | |
bleomycin A2 + H2O | recombinant enzyme shows rapid and efficient hydrolysis of all bleomycins tested, exhibiting a superior catalytic efficiency for bleomycin B2 | Homo sapiens | deamido bleomycin A2 + NH3 | - |
? | |
bleomycin B2 + H2O | the enzyme hydrolyzes bleomycins into the biologically inactive deamido bleomycins | Homo sapiens | deamido bleomycin B2 + NH3 | - |
? | |
bleomycin B2 + H2O | recombinant enzyme shows rapid and efficient hydrolysis of all bleomycins tested, exhibiting a superior catalytic efficiency for bleomycin B2 | Homo sapiens | deamido bleomycin B2 + NH3 | - |
? | |
bleomycin Z + H2O | recombinant enzyme shows rapid and efficient hydrolysis of all bleomycins tested, exhibiting a superior catalytic efficiency for bleomycin B2 | Homo sapiens | deamido bleomycin Z + NH3 | - |
? | |
tallysomycin H1 + H2O | - |
Homo sapiens | ? + NH3 | - |
? |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
2.4 | - |
tallysomycin H1 | pH 7.5, 30°C | Homo sapiens | |
2.5 | - |
6'-deoxy tallysomycin H1 | pH 7.5, 30°C | Homo sapiens | |
4 | - |
bleomycin A2 | pH 7.5, 30°C | Homo sapiens | |
4.9 | - |
6'-deoxy bleomycin A2 | pH 7.5, 30°C | Homo sapiens | |
9.8 | - |
bleomycin Z | pH 7.5, 30°C | Homo sapiens | |
11 | - |
bleomycin B2 | pH 7.5, 30°C | Homo sapiens | |
15 | - |
6'-deoxy bleomycin Z | pH 7.5, 30°C | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
3.2 | - |
tallysomycin H1 | pH 7.5, 30°C | Homo sapiens | |
3.5 | - |
6'-deoxy tallysomycin H1 | pH 7.5, 30°C | Homo sapiens | |
6.1 | - |
6'-deoxy bleomycin A2 | pH 7.5, 30°C | Homo sapiens | |
6.7 | - |
bleomycin A2 | pH 7.5, 30°C | Homo sapiens | |
11 | - |
bleomycin Z | pH 7.5, 30°C | Homo sapiens | |
16 | - |
6'-deoxy bleomycin Z | pH 7.5, 30°C | Homo sapiens | |
58 | - |
bleomycin B2 | pH 7.5, 30°C | Homo sapiens |