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Literature summary for 2.7.4.9 extracted from

  • Chen, M.D.; Sinha, K.; Rule, G.S.; Ly, D.H.
    Interaction of alpha-thymidine inhibitors with thymidylate kinase from Plasmodium falciparum (2018), Biochemistry, 57, 2868-2875 .
    View publication on PubMed
Search for more literature for 2.7.4.9

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Plasmodium falciparum

Protein Variants

Protein Variants Comment Organism
F74A mutant enzyme has no enzymatic activity Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
1-[2,5-dideoxy-5-[([4-[(2-fluorophenyl)methoxy]phenyl]carbamoyl)amino]-alpha-D-erythro-pentofuranosyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
 Plasmodium falciparum
1-[2,5-dideoxy-5-[([4-[(2-methoxyphenyl)methoxy]phenyl]carbamoyl)amino]-alpha-D-erythro-pentofuranosyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
 Plasmodium falciparum
1-[5-[([4-[(2-chlorophenyl)methoxy]phenyl]carbamoyl)amino]-2,5-dideoxy-alpha-D-erythro-pentofuranosyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
 Plasmodium falciparum
N-(5'-deoxy-alpha-thymidin-5'-yl)-N'-[4-(2-chlorobenzyloxy)phenyl]urea
-
 Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q8I4S1
-
-
Plasmodium falciparum isolate 3D7 Q8I4S1
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + dTMP
-
 Plasmodium falciparum ADP + dTDP
-
 ?
ATP + dTMP
-
 Plasmodium falciparum isolate 3D7 ADP + dTDP
-
 ?

Synonyms

Synonyms Comment Organism
thymidylate kinase
-
 Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0205
-
 1-[2,5-dideoxy-5-[([4-[(2-fluorophenyl)methoxy]phenyl]carbamoyl)amino]-alpha-D-erythro-pentofuranosyl]-5-methylpyrimidine-2,4(1H,3H)-dione pH and temperature not specified in the publication Plasmodium falciparum
0.22
-
 1-[2,5-dideoxy-5-[([4-[(2-methoxyphenyl)methoxy]phenyl]carbamoyl)amino]-alpha-D-erythro-pentofuranosyl]-5-methylpyrimidine-2,4(1H,3H)-dione pH and temperature not specified in the publication Plasmodium falciparum
0.225
-
 1-[5-[([4-[(2-chlorophenyl)methoxy]phenyl]carbamoyl)amino]-2,5-dideoxy-alpha-D-erythro-pentofuranosyl]-5-methylpyrimidine-2,4(1H,3H)-dione pH and temperature not specified in the publication Plasmodium falciparum

General Information

General Information Comment Organism
physiological function critical enzyme in the de novo biosynthesis pathway of pyrimidine nucleotides Plasmodium falciparum