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Literature summary for 2.1.1.45 extracted from

  • Kawate, H.; Landis, D.M.; Loeb, L.A.
    Distribution of mutations in human thymidylate synthase yielding resistance to 5-fluorodeoxyuridine (2002), J. Biol. Chem., 277, 36304-36311.
    View publication on PubMed

Application

Application Comment Organism
medicine enzyme is believed to be the major site of the cytotoxic action of the cancer chemotherapeutic drug 5-fluorouracil, development of inhibitors as clinical useful drugs Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
Escherichia coli NM522 cells used for cloning and library construction, Escherichia coli chi2913recA lacking TS used for expression by complementation Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0007
-
2'-deoxyuridylate mutant 362(T51S,K82Q,N171S) Homo sapiens
0.001
-
2'-deoxyuridylate mutant Y258F Homo sapiens
0.0011
-
2'-deoxyuridylate mutant 302(T53S,Y258F) Homo sapiens
0.002
-
2'-deoxyuridylate wild type Homo sapiens
0.0026
-
2'-deoxyuridylate mutant T51S Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
72000
-
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5,10-methylenetetrahydrofolate + dUMP Homo sapiens biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism dihydrofolate + dTMP
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P04818 human
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzyme Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
bone marrow
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(6R)-N5,N10-methylene-5,6,7,8-tetrahydrofolate + 2'-deoxyuridylate
-
Homo sapiens 7,8-dihydrofolate + 5-methyl-2'-deoxyuridylate
-
r
5,10-methylenetetrahydrofolate + dUMP
-
Homo sapiens dihydrofolate + dTMP
-
r
5,10-methylenetetrahydrofolate + dUMP biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism Homo sapiens dihydrofolate + dTMP
-
?

Subunits

Subunits Comment Organism
dimer homodimer Homo sapiens