(Q40872442)

24 September 2017

1 reference

title

Thymidylate synthase inhibition: a structure-based rationale for drug design (English)

1 reference

24 September 2017

Costi MP

1

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24 September 2017

publication date

1 January 1998

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Medicinal Research Reviews

24 September 2017

published in

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24 September 2017

volume

18

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24 September 2017

issue

1

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24 September 2017

page(s)

21-42

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The thymidylate synthesis cycle and anticancer drugs

24 September 2017

cites work

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Site-directed mutagenesis of varicella-zoster virus thymidylate synthase. Analysis of two highly conserved regions of the enzyme

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Splicing signals are required for S-phase regulation of the mouse thymidylate synthase gene

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Thymidylate synthase mRNA level in adenocarcinoma of the stomach: a predictor for primary tumor response and overall survival

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Crystal structure of human thymidylate synthase: a structural mechanism for guiding substrates into the active site

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Plastic adaptation toward mutations in proteins: structural comparison of thymidylate synthases

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

The catalytic mechanism and structure of thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Atomic structure of thymidylate synthase: target for rational drug design

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Refined structures of substrate-bound and phosphate-bound thymidylate synthase from Lactobacillus casei

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Structure of and kinetic channelling in bifunctional dihydrofolate reductase-thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Crystal structure of thymidylate synthase from T4 phage: component of a deoxynucleoside triphosphate-synthesizing complex

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Structural basis for recognition of polyglutamyl folates by thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Roles of Cys148 and Asp179 in catalysis by deoxycytidylate hydroxymethylase from bacteriophage T4 examined by site-directed mutagenesis

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Pairwise specificity and sequential binding in enzyme catalysis: thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Partitioning roles of side chains in affinity, orientation, and catalysis with structures for mutant complexes: asparagine-229 in thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Design of enzyme inhibitors using iterative protein crystallographic analysis

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Design and synthesis of novel 6,7-imidazotetrahydroquinoline inhibitors of thymidylate synthase using iterative protein crystal structure analysis

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Structure-based discovery of inhibitors of thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Crystal-structure-based design and synthesis of benz[cd]indole-containing inhibitors of thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Exclusion of 2'-deoxycytidine 5'-monophosphate by asparagine 229 of thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

5-Fluoro-2'-deoxycytidine 5'-monophosphate is a mechanism-based inhibitor of thymidylate synthase.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Asparagine 229 in thymidylate synthase contributes to, but is not essential for, catalysis

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Design and synthesis of a helix heparin-binding peptide

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Asparagine 229 mutants of thymidylate synthase catalyze the methylation of 3-methyl-2'-deoxyuridine 5'-monophosphate.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Substitution of glutamine for glutamic acid-58 in Escherichia coli thymidylate synthase results in pronounced decreases in catalytic activity and ligand binding.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Role of the conserved tryptophan 82 of Lactobacillus casei thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

The effect of substrate analogs on the circular dichroic spectra of thymidylate synthetase from Lactobacillus casei

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Complete restoration of activity to inactive mutants of Escherichia coli thymidylate synthase: evidence that E. coli thymidylate synthase is a half-the-sites activity enzyme.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Mechanism-based inhibition of thymidylate synthase by 5-(trifluoromethyl)-2'-deoxyuridine 5'-monophosphate

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Trans-5-(3,3,3-trifluoro-1-propenyl)-2'-deoxyuridylate: a mechanism-based inhibitor of thymidylate synthetase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Interaction of thymidylate synthase with pyridoxal 5'-phosphate as studied by UV/visible difference spectroscopy and molecular modeling

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Interaction of 1-(5-phospho-.beta.-D-arabinofuranosyl)-5-substituted-uracils with thymidylate synthetase: mechanism-based inhibition by 1-(5-phospho-.beta.-D-arabinofurosyl)-5-fluorouracil

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Classical and nonclassical furo[2,3-d]pyrimidines as novel antifolates: synthesis and biological activities

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Entropy in bi-substrate enzymes: proposed role of an alternate site in chaperoning substrate into, and products out of, thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Folate analogues. 21. Synthesis and antifolate and antitumor activities of N10-(cyanomethyl)-5,8-dideazafolic acid

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Folate analogues. 26. Syntheses and antifolate activity of 10-substituted derivatives of 5,8-dideazafolic acid and of the poly-gamma-glutamyl metabolites of N10-propargyl-5,8-dideazafolic acid (PDDF).

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Folate analogues. 30. Synthesis and biological evaluation of N10-propargyl-5,8-dideaza-5,6,7,8-tetrahydrofolic acid and related compounds

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Folate analogues as inhibitors of thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Potent inhibition of thymidylate synthase by two series of nonclassical quinazolines

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Quinazoline antifolate thymidylate synthase inhibitors: bridge modifications and conformationally restricted analogues in the C2-methyl series

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

A dideazatetrahydrofolate analogue lacking a chiral center at C-6, N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5- yl)ethyl]benzoyl]-L-glutamic acid, is an inhibitor of thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Effect of bridge region variation on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Application of the three-dimensional structures of protein target molecules in structure-based drug design

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Synthesis and biological evaluation of novel 2,6-diaminobenz[cd]indole inhibitors of thymidylate synthase using the protein structure as a guide

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Structure-based design of lipophilic quinazoline inhibitors of thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Structure-based strategies for drug design and discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

The art and practice of structure-based drug design: A molecular modeling perspective

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Quinazoline antifolate thymidylate synthase inhibitors: replacement of glutamic acid in the C2-methyl series

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Structure-based design of substituted diphenyl sulfones and sulfoxides as lipophilic inhibitors of thymidylate synthase.

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Quinazoline antifolates with dual biochemical loci of action. Biochemical and biological studies directed towards overcoming methotrexate resistance

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Mechanism-based inhibitors of thymidylate synthetase

21 January 2018

1 reference

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Thymidylate synthase as a target in cancer chemotherapy

21 January 2018

1 reference

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Catalytic function of thymidylate synthase is confined to S phase due to its association with replitase

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Crystal structure of Escherichia coli thymidylate synthase containing bound 5-fluoro-2'-deoxyuridylate and 10-propargyl-5,8-dideazafolate

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Sulphonamide antifolates inhibiting thymidylate synthase: synthesis, enzyme inhibition and cytotoxicity

21 January 2018

1 reference

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Nucleosides and nucleotides. 97. Synthesis of new broad spectrum antineoplastic nucleosides, 2'-deoxy-2'-methylidenecytidine (DMDC) and its derivatives

21 January 2018

1 reference

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Inhibition of thymidylate synthetase by 5-alkynyl-2'-deoxyuridylates

21 January 2018

1 reference

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Use of 10-propargyl-5,8-dideazafolate and directed mutagenesis to probe the catalytic mechanism of thymidylate synthase.

21 January 2018

1 reference

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Quinoline antifolate thymidylate synthase inhibitors: variation of the C2- and C4-substituents

21 January 2018

1 reference

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Quinazoline antifolates thymidylate synthase inhibitors: lipophilic analogues with modification to the C2-methyl substituent

21 January 2018

1 reference

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Quinazoline antifolate thymidylate synthase inhibitors: difluoro-substituted benzene ring analogs

21 January 2018

1 reference

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Quinazoline antifolates inhibiting thymidylate synthase: 2-desamino derivatives with enhanced solubility and potency

21 January 2018

1 reference

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Comparison of the biological effects of selected 5,8-dideazafolate analogues with their 2-desamino counterparts

21 January 2018

1 reference

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Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some sulfonamidobenzoylglutamate and related derivatives

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

5-Arylthio-substituted 2-amino-4-oxo-6-methylpyrrolo[2,3-d]pyrimidine antifolates as thymidylate synthase inhibitors and antitumor agents

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Quinazoline antifolate thymidylate synthase inhibitors: gamma-linked L-D, D-D, and D-L dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583)

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Naphthalimido derivatives as antifolate thymidylate synthase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Conformational analysis of phthalein derivatives acting as thymidylate synthase inhibitors by means of 1H NMR and quantum chemical calculations

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

Thymidylate synthase inhibition, a dead end?

21 January 2018

1 reference

https://api.crossref.org/works/10.1002%2F%28SICI%291098-1128%28199801%2918%3A1%3C21%3A%3AAID-MED2%3E3.0.CO%3B2-U

10.1002/(SICI)1098-1128(199801)18:1<21::AID-MED2>3.0.CO;2-U

21 January 2018

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DOI

1 reference

24 September 2017

1 reference