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CB 3717

Known as: CB-3717, CB3717 
National Institutes of Health

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6 relations

Broader (5)

Antineoplastic AgentsEnzyme InhibitorsFolic AcidFolic Acid Antagonists
analogs & derivatives

Papers overview

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2002
2002
Tryptophan 80 and leucine 143 are critical for the hydride transfer step of thymidylate synthase by controlling active site access.
Mutant forms of thymidylate synthase (TS) with substitutions at the conserved active site residue, Trp 80, are deficient in the… 
1996
1996
Unusual binding stoichiometries and cooperativity are observed during binary and ternary complex formation in the single active pore of R67 dihydrofolate reductase, a D2 symmetric protein.
R67 dihydrofolate reductase (DHFR) is an R-plasmid-encoded enzyme that confers resistance to the antibacterial drug, trimethoprim… 
1996
1996
Structure-based design of lipophilic quinazoline inhibitors of thymidylate synthase.
To develop novel lipophilic thymidylate synthase (TS) inhibitors, the X-ray structure of Escherichia coli TS in ternary complex… 
Review
1994
Review
1994
The antitumour activity of ZD9331, a non-polyglutamatable quinazoline thymidylate synthase inhibitor.
Thymidylate synthase (TS) is regarded as a good target for the development of quinazoline (folate-based) anticancer agents. The… 
Highly Cited
1992
Highly Cited
1992
Cofactor triggers the conformational change in thymidylate synthase: implications for an ordered binding mechanism.
We have solved crystal structures of two complexes with Escherichia coli thymidylate synthase (TS) bound either to the cofactor… 
1991
1991
Interaction between 5-fluorouracil, [6RS]leucovorin, and recombinant human interferon-alpha 2a in cultured colon adenocarcinoma cells.
Recombinant human interferon-alpha 2a (rIFN-alpha 2a; 500 or 5,000 IU/mL) or [6RS] leucovorin ([6RS]LV; 1 microM) each… 
1987
1987
Recent preclinical and clinical studies with the thymidylate synthase inhibitor N10-propargyl-5,8-dideazafolic acid (CB 3717).
CB 3717, N10-propargyl-5,8-dideazafolic acid, is a tight-binding inhibitor of thymidylate synthase (TS) whose cytotoxicity is… 
Highly Cited
1983
Highly Cited
1983
Patterns of cross-resistance to the antifolate drugs trimetrexate, metoprine, homofolate, and CB3717 in human lymphoma and osteosarcoma cells resistant to methotrexate.
Methotrexate (MTX)-resistant sublines of malignant human cells were selected in vitro by stepwise increase in drug concentration… 
Highly Cited
1983
Highly Cited
1983
Biochemical effects of a quinazoline inhibitor of thymidylate synthetase, N-(4-(N-((2-amino-4-hydroxy-6-quinazolinyl)methyl)prop-2-ynylamino)benzoyl)-l-glutamic acid (CB3717), on human lymphoblastoid…
1983
1983
Biochemical effects of a quinazoline inhibitor of thymidylate synthetase, N-(4-(N-(( 2-amino-4-hydroxy-6-quinazolinyl)methyl)prop-2-ynylamino) benzoyl)-L-glutamic acid (CB3717), on human…
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