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Literature summary for 2.1.2.2 extracted from

  • Habeck, L.L.; Leitner, T.A.; Shackelford, K.A.; Gossett, L.S.; Schultz, R.M.; Andis, S.L.; Shih, C.; Grindey, G.B.; Mendelsohn, L.G.
    A novel class of monoglutamated antifolates exhibits tight-binding inhibition of human glycinamide ribonucleotide formyltransferase and potent activity against solid tumors (1994), Cancer Res., 54, 1021-1026.
    View publication on PubMed
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Application

Application Comment Organism
medicine
-
 Homo sapiens
medicine inhibitor 5,10-dideazatetrahydrofolate is antiproliferate and cytotoxic against mammalian tumor cells in culture and have broad spectrum activity against transplantable mouse tumors and human tumor xenografts Mus musculus

Cloned(Commentary)

Cloned (Comment) Organism
cloned and expressed in Escherichia coli BL21(DE3)pLysS Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(6R)-5,10-dideazatetrahydrofolate lometrexol Homo sapiens
(6R)-dideazatetrahydrofolate diglutamate LY235340 Homo sapiens
(6R)-dideazatetrahydrofolate diglutamate LY235340 Mus musculus
(6R)-dideazatetrahydrofolate pentaglutamate LY235542 Homo sapiens
(6R)-dideazatetrahydrofolate pentaglutamate LY235542 Mus musculus
(6R)-dideazatetrahydrofolate tetraglutamate LY266978 Homo sapiens
(6R)-dideazatetrahydrofolate tetraglutamate LY266978 Mus musculus
(6R)-dideazatetrahydrofolate triglutamate LY235337 Homo sapiens
(6R)-dideazatetrahydrofolate triglutamate LY235337 Mus musculus
(6S)-dideazatetrahydrofolate LY243246 Homo sapiens
(6S)-dideazatetrahydrofolate LY243246 Mus musculus
2',5'-furan-dideazatetrahydrofolate LY222306 Homo sapiens
2',5'-furan-dideazatetrahydrofolate LY222306 Mus musculus
2',5'-thiophene dideazatetrahydrofolate LY309886, diastereomer A; LY309887, diastereomer B Homo sapiens
2',5'-thiophene dideazatetrahydrofolate LY309886, diastereomer A; LY309887, diastereomer B Mus musculus
5,10-dideazatetrahydrofolate
-
 Homo sapiens
5,10-dideazatetrahydrofolate
-
 Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide Mus musculus
-
 tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
 ?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide Homo sapiens
-
 tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 human
-
Mus musculus
-
 mouse
-

Purification (Commentary)

Purification (Comment) Organism
-
 Mus musculus

Source Tissue

Source Tissue Comment Organism Textmining
colonic cancer cell xenograft HXGC3, HC1 and VRC5 Homo sapiens
-
lymphosarcoma cell 6C3HED Mus musculus
-
mammary carcinoma cell 3CH Mus musculus
-
PANC-1 cell xenograft, pancreatic carcinoma Homo sapiens
-
pancreas
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
-
 Mus musculus tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
 ?
10-formyltetrahydrofolate + 5-phospho-D-ribosylglycinamide
-
 Homo sapiens tetrahydrofolate + 5'-phosphoribosyl-N-formylglycinamide
-
 ?