Promotion of purine nucleotide binding to thymidylate synthase by a potent folate analogue inhibitor, 1843U89.

No abstract is available for this paper.

• Publication year

  1995

• Venue

  Proceedings of the National Academy of Sciences of the United States of America

• Publication date

  1995-04-11

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1073/PNAS.92.8.3493PMID 7724588PMCID PMC42193
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• The clinical pharmacokinetics of the novel antifolate N10-propargyl-5,8-dideazafolic acid (CB 3717)

  2004cited by this paper
• Water-mediated substrate/product discrimination: the product complex of thymidylate synthase at 1.83 A.

  1994cited by this paper
• Mode of binding of folate analogs to thymidylate synthase. Evidence for two asymmetric but interactive substrate binding sites.

  1994cited by this paper
• Biochemical and cellular pharmacology of 1843U89, a novel benzoquinazoline inhibitor of thymidylate synthase.

  1993cited by this paper
• Refined structures of substrate-bound and phosphate-bound thymidylate synthase from Lactobacillus casei.

  1993cited by this paper
• Cofactor triggers the conformational change in thymidylate synthase: implications for an ordered binding mechanism.

  1992cited by this paper
• Crystal structure of Escherichia coli thymidylate synthase containing bound 5-fluoro-2'-deoxyuridylate and 10-propargyl-5,8-dideazafolate.

  1990cited by this paper
• An ultrafiltration assay for nucleotide binding to ribonucleotide reductase.

  1990cited by this paper
• Stereochemical mechanism of action for thymidylate synthase based on the X-ray structure of the covalent inhibitory ternary complex with 5-fluoro-2'-deoxyuridylate and 5,10-methylenetetrahydrofolate.

  1990cited by this paper
• Structure, multiple site binding, and segmental accommodation in thymidylate synthase on binding dUMP and an anti-folate.

  1990cited by this paper
• Properties of a defined mutant of Escherichia coli thymidylate synthase.

  1988cited by this paper
• A potent antitumour quinazoline inhibitor of thymidylate synthetase: synthesis, biological properties and therapeutic results in mice.

  1981cited by this paper
• Fluorine-19 nuclear magnetic resonance investigation of the noncovalent and covalent binary complexes of 5-fluorodeoxyuridylate and Lactobacillus casei thymidylate synthetase.

  1980cited by this paper
• A calorimetric study of the binding of 2'-deoxyuridine-5'-phosphate and its analogs to thymidylate synthetase.

  1980cited by this paper
• Evidence for a sequential interaction of the subunits of thymidylate synthetase.

  1979cited by this paper
• Differential inhibition of host and viral thymidylate synthetases by folylpolyglutamates.

  1979cited by this paper
• Thymidylate synthetase and 2'-deoxyuridylate form a tight complex in the presence of pteroyltriglutamate.

  1979cited by this paper
• Protective effect of the pteroylpolyglutamates and phosphate on the proteolytic inactivation of thymidylate synthetase.

  1977cited by this paper
• Factors affecting substrate binding in Lactobacillus casei thymidylate synthetase as studied by equilibrium dialysis.

  1976cited by this paper
• Demonstration of separate binding sites for the folate coenzymes and deoxynucleotides with inactivated Lactobacillus casei thymidylate synthetase.

  1976cited by this paper
• The effect of substrate analogs on the circular dichroic spectra of thymidylate synthetase from Lactobacillus casei.

  1975cited by this paper
• Interaction of deoxyuridylate with thymidylate synthetase.

  1975cited by this paper
• Thymidylate synthetase: mechanism of inhibition by 5-fluoro-2'-deoxyuridylate.

  1972cited by this paper
• 5-Fluoro-2'-deoxyuridylate: covalent complex with thymidylate synthetase.

  1972cited by this paper
• Fluorinated pyrimidines. XL. The reduction of 5-fluorouridine 5'-diphosphate by ribonucleotide reductase.

  1972cited by this paper
• The purification and properties of thymidylate synthetase from chick embryo extracts.

  1967cited by this paper
• Studies on fluorinated pyrimidines. XIII. Inhibition of thymidylate synthetase.

  1961cited by this paper
• THE MODE OF ACTION OF 5-FLUOROURACIL AND ITS DERIVATIVES.

  1958cited by this paper

• Human Thymidylate Synthase Inhibitors Halting Ovarian Cancer Growth.

  2018cites this paper
• Design, synthesis, biological evaluation and X-ray crystal structure of novel classical 6,5,6-tricyclic benzo[4,5]thieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.

  2011cites this paper
• Targeting the DNA damage response in cancer.

  2009cites this paper
• Role of an invariant lysine residue in folate binding on Escherichia coli thymidylate synthase: calorimetric and crystallographic analysis of the K48Q mutant.

  2008cites this paper
• Role of thymidine phosphorylase/platelet-derived endothelial cell growth factor inhibition in the cytotoxicity of fluoropyrimidines

  2007cites this paper
• Thymidylate synthase inhibitors.

  2006influential citation
• Novel chemical strategies for thymidylate synthase inhibition.

  2005cites this paper
• Low folate conditions may enhance the interaction of trifluorothymidine with antifolates in colon cancer cells

  2005cites this paper
• Virtual screening of human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase against the NCI diversity set by use of AutoDock to identify novel nonfolate inhibitors.

  2004cites this paper
• Relative free energies of binding to thymidylate synthase of 2- and/or 4-thio and/or 5-fluoro analogues of dUMP

  2003cites this paper
• Deaza analogs of folic acid as antitumor agents.

  2003cites this paper
• Effects of antifolates on the binding of 5-fluoro-2'-deoxyuridine monophosphate to thymidylate synthase.

  2002cites this paper
• Thymidylate synthase inhibitors.

  2001influential citation
• Parameters affecting the restoration of activity to inactive mutants of thymidylate synthase via subunit exchange: further evidence that thymidylate synthase is a half-of-the-sites activity enzyme.

  2001cites this paper
• High-level expression of Escherichia coli and Bacillus subtilis thymidylate synthases.

  2000cites this paper
• Thymidylate synthase inhibitors.

  1999influential citation
• Thymidylate synthase inhibition: A structure‐based rationale for drug design

  1998cites this paper
• Mode of action of site-directed irreversible folate analogue inhibitors of thymidylate synthase.

  1998cites this paper
• Probing the Folate-binding Site of Human Thymidylate Synthase by Site-directed Mutagenesis

  1998cites this paper
• Use of strain in a stereospecific catalytic mechanism: crystal structures of Escherichia coli thymidylate synthase bound to FdUMP and methylenetetrahydrofolate.

  1997cites this paper
• Thymidylate synthase: structure, inhibition, and strained conformations during catalysis.

  1997cites this paper
• Thermodynamic stabilization of nucleotide binding to thymidylate synthase by a potent benzoquinazoline folate analogue inhibitor.

  1996cites this paper
• Thymidylate synthase inhibitors.

  1996influential citation
• The complex of the anti-cancer therapeutic, BW1843U89, with thymidylate synthase at 2.0 A resolution: implications for a new mode of inhibition.

  1996cites this paper
• Ligand-induced distortion of an active site in thymidylate synthase upon binding anticancerdrug 1843U89

  1995cites this paper
• Structural aspects of the inhibition and catalytic mechanism of thymidylate synthase.

  1995cites this paper