CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil

[1]  G. Superti-Furga,et al.  Proteome-wide drug and metabolite interaction mapping by thermal-stability profiling , 2015, Nature Methods.

[2]  G. Drewes,et al.  Thermal proteome profiling for unbiased identification of direct and indirect drug targets using multiplexed quantitative mass spectrometry , 2015, Nature Protocols.

[3]  John P. Overington,et al.  The promise and peril of chemical probes. , 2015, Nature chemical biology.

[4]  G. Peters,et al.  Inhibition of thymidylate synthase by 2',2'-difluoro-2'-deoxycytidine (Gemcitabine) and its metabolite 2',2'-difluoro-2'-deoxyuridine. , 2015, The international journal of biochemistry & cell biology.

[5]  M. Blanco,et al.  Target engagement in lead generation. , 2015, Bioorganic & medicinal chemistry letters.

[6]  A. Lavie,et al.  Structure-Guided Development of Deoxycytidine Kinase Inhibitors with Nanomolar Affinity and Improved Metabolic Stability , 2014, Journal of medicinal chemistry.

[7]  G. Drewes,et al.  Tracking cancer drugs in living cells by thermal profiling of the proteome , 2014, Science.

[8]  P. Nordlund,et al.  The cellular thermal shift assay for evaluating drug target interactions in cells , 2014, Nature Protocols.

[9]  M. Pangalos,et al.  Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework , 2014, Nature Reviews Drug Discovery.

[10]  P. Johnston,et al.  Standing the test of time: targeting thymidylate biosynthesis in cancer therapy , 2014, Nature Reviews Clinical Oncology.

[11]  P. Artursson,et al.  A High-Throughput Cell-Based Method to Predict the Unbound Drug Fraction in the Brain , 2014, Journal of medicinal chemistry.

[12]  P. Nordlund,et al.  Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay , 2013, Science.

[13]  Per Artursson,et al.  Rapid measurement of intracellular unbound drug concentrations. , 2013, Molecular pharmaceutics.

[14]  Mark E Bunnage,et al.  Target validation using chemical probes. , 2013, Nature chemical biology.

[15]  B. Cravatt,et al.  Determining target engagement in living systems. , 2013, Nature chemical biology.

[16]  Yehuda G Assaraf,et al.  Antifolates in cancer therapy: structure, activity and mechanisms of drug resistance. , 2012, Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy.

[17]  Paul Morgan,et al.  Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival. , 2012, Drug discovery today.

[18]  F. Lyko,et al.  Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine , 2008, International journal of cancer.

[19]  F. Niesen,et al.  The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability , 2007, Nature Protocols.

[20]  Y. Assaraf.  Molecular basis of antifolate resistance , 2007, Cancer and Metastasis Reviews.

[21]  Masoud Vedadi,et al.  Screening for Ligands Using a Generic and High-Throughput Light-Scattering-Based Assay , 2006, Journal of biomolecular screening.

[22]  George T Detitta,et al.  Thermofluor-based high-throughput stability optimization of proteins for structural studies. , 2006, Analytical biochemistry.

[23]  R. Momparler.  Pharmacology of 5-Aza-2'-deoxycytidine (decitabine). , 2005, Seminars in hematology.

[24]  G. Peters,et al.  Intracellular Thymidylate Synthase Inhibition by Trifluorothymidine in FM3A Cells , 2004, Nucleosides, nucleotides & nucleic acids.

[25]  C. Lipinski.  Lead- and drug-like compounds: the rule-of-five revolution. , 2004, Drug discovery today. Technologies.

[26]  P. Johnston,et al.  5-Fluorouracil: mechanisms of action and clinical strategies , 2003, Nature Reviews Cancer.

[27]  S. B. Gates,et al.  Multi-targeted antifolates aimed at avoiding drug resistance form covalent closed inhibitory complexes with human and Escherichia coli thymidylate synthases. , 2001, Journal of molecular biology.

[28]  G. Maley,et al.  Crystal structure of a deletion mutant of human thymidylate synthase Δ (7–29) and its ternary complex with Tomudex and dUMP , 2001, Protein science : a publication of the Protein Society.

[29]  Thomas D. Y. Chung,et al.  A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays , 1999, Journal of biomolecular screening.

[30]  J. Houghton,et al.  Ratio of 2'-deoxyadenosine-5'-triphosphate/thymidine-5'-triphosphate influences the commitment of human colon carcinoma cells to thymineless death. , 1995, Clinical cancer research : an official journal of the American Association for Cancer Research.

[31]  J. Finer-Moore,et al.  Mechanism-based inhibition of thymidylate synthase by 5-(trifluoromethyl)-2'-deoxyuridine 5'-monophosphate. , 1994, Biochemistry.

[32]  J. Hickman,et al.  bcl-2 modulation of apoptosis induced by anticancer drugs: resistance to thymidylate stress is independent of classical resistance pathways. , 1993, Cancer research.

[33]  Acknowledgements , 1992, Experimental Gerontology.

[34]  Ralph H. Johnson,et al.  Drugs and Folate Metabolism , 1985, Drugs.

[35]  A. M. Shestopalov,et al.  New method of synthesis of substituted 2-pyridones , 1984 .

[36]  M. Rossi,et al.  Kinetic interaction of 5-AZA-2'-deoxycytidine-5'-monophosphate and its 5'-triphosphate with deoxycytidylate deaminase. , 1984, Molecular pharmacology.

[37]  R. Momparler,et al.  Kinetics of deamination of 5-aza-2'-deoxycytidine and cytosine arabinoside by human liver cytidine deaminase and its inhibition by 3-deazauridine, thymidine or uracil arabinoside. , 1983, Biochemical pharmacology.

[38]  R. T. Walker,et al.  Thymidylate synthetase as target enzyme for the inhibitory activity of 5-substituted 2'-deoxyuridines on mouse leukemia L1210 cell growth. , 1981, Molecular pharmacology.

[39]  C. Heidelberger,et al.  Structures of reversible and irreversible complexes of thymidylate synthetase and fluorinated pyrimidine nucleotides. , 1974, Biochemistry.

[40]  I. Ial,et al.  Nature Communications , 2010, Nature Cell Biology.

[41]  Joseph D. Kwasnoski,et al.  High-density miniaturized thermal shift assays as a general strategy for drug discovery. , 2001, Journal of biomolecular screening.

[42]  R. Momparler.  Molecular, cellular and animal pharmacology of 5-aza-2'-deoxycytidine. , 1985, Pharmacology & therapeutics.

[43]  P. Danenberg,et al.  Fluorinated pyrimidines as tight-binding inhibitors of thymidylate synthetase. , 1981, Pharmacology & therapeutics.