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Literature summary for 3.4.22.40 extracted from

  • Crnovcic, I.; Gan, F.; Yang, D.; Dong, L.B.; Schultz, P.G.; Shen, B.
    Activities of recombinant human bleomycin hydrolase on bleomycins and engineered analogues revealing new opportunities to overcome bleomycin-induced pulmonary toxicity (2018), Bioorg. Med. Chem. Lett., 28, 2670-2674 .
    View publication on PubMed
Search for more literature for 3.4.22.40

Application

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(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Homo sapiens

KM Value [mM]

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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens Q13867
-
-

Source Tissue

Source Tissue Comment Organism Textmining
lung poorly expressed in the lung Homo sapiens
-

Substrates and Products (Substrate)

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 [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
 assay at Homo sapiens

Turnover Number [1/s]

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

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens

kcat/KM [mM/s]

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