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Literature summary for 3.5.4.4 extracted from

  • Tyler, P.C.; Taylor, E.A.; Froehlich, R.F.; Schramm, V.L.
    Synthesis of 5-methylthio coformycins: specific inhibitors for malarial adenosine deaminase (2007), J. Am. Chem. Soc., 129, 6872-6879.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
pharmacology Plasmodium falciparum-specific inhibitors of adenosine deaminase have potential for development as antimalarials without inhibition of host enzyme Plasmodium falciparum

Cloned(Commentary)

Cloned (Comment) Organism
expression of His-tagged enzyme in Escherichia coli strain BL21 Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
2'-deoxycoformycin a natural product transition state analogue inhibitor Bos taurus
2'-deoxycoformycin a natural product transition state analogue inhibitor Homo sapiens
2'-deoxycoformycin a natural product transition state analogue inhibitor Plasmodium falciparum
5'-methylthio-2'-deoxycoformycin
-
Plasmodium falciparum
5'-methylthiocoformycin
-
Plasmodium falciparum
coformycin a natural product transition state analogue inhibitor Bos taurus
coformycin a natural product transition state analogue inhibitor Homo sapiens
coformycin a natural product transition state analogue inhibitor Plasmodium falciparum
additional information no inhibition of the bovine enzyme by 5'-methylthiocoformycin and 5'-methylthio-2'-deoxycoformycin Bos taurus
additional information no inhibition of the human enzyme by 5'-methylthiocoformycin and 5'-methylthio-2'-deoxycoformycin Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5'-methylthioadenosine + H2O Plasmodium falciparum
-
5'-methylthioinosine + NH3
-
?
adenosine + H2O Homo sapiens
-
inosine + NH3
-
?
adenosine + H2O Bos taurus
-
inosine + NH3
-
?
adenosine + H2O Plasmodium falciparum adenosine deamination is involved in the essential pathway of purine salvage in Plasmodium falciparum, and inhibition of purine salvage results in parasite death inosine + NH3
-
?

Organism

Organism UniProt Comment Textmining
Bos taurus
-
calf
-
Homo sapiens
-
-
-
Plasmodium falciparum
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged enzyme from Escherichia coli strain BL21 by nickel affinity chromatography Plasmodium falciparum

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Homo sapiens
-
commercial preparation
-
Bos taurus
-
erythrocyte
-
Homo sapiens
-
spleen
-
Bos taurus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5'-methylthioadenosine + H2O
-
Plasmodium falciparum 5'-methylthioinosine + NH3
-
?
adenosine + H2O
-
Homo sapiens inosine + NH3
-
?
adenosine + H2O
-
Bos taurus inosine + NH3
-
?
adenosine + H2O
-
Plasmodium falciparum inosine + NH3
-
?
adenosine + H2O adenosine deamination is involved in the essential pathway of purine salvage in Plasmodium falciparum, and inhibition of purine salvage results in parasite death Plasmodium falciparum inosine + NH3
-
?
additional information no activity with 5'-methylthioadenosine Homo sapiens ?
-
?
additional information no activity with 5'-methylthioadenosine Bos taurus ?
-
?

Synonyms

Synonyms Comment Organism
ADA
-
Homo sapiens
ADA
-
Bos taurus
ADA
-
Plasmodium falciparum

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Homo sapiens
30
-
assay at Bos taurus
30
-
assay at Plasmodium falciparum

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
assay at Homo sapiens
7
-
assay at Bos taurus
7
-
assay at Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000043
-
5'-methylthiocoformycin
-
Plasmodium falciparum
0.00000079
-
5'-methylthio-2'-deoxycoformycin
-
Plasmodium falciparum