Pyrimidine nucleotide biosynthesis in animals: genes, enzymes, and regulation of UMP biosynthesis, Annu Rev Biochem, vol.49, pp.253-79, 1980. ,
Structure-based design, synthesis, and characterization of inhibitors of human and Plasmodium falciparum dihydroorotate dehydrogenases, J Med Chem, vol.52, pp.2683-93, 2009. ,
Novel inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with anti-malarial activity in the mouse model, J Biol Chem, vol.285, pp.33054-64, 2010. ,
Structure-guided lead optimization of triazolopyrimidinering substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential, J Med Chem, vol.54, pp.5540-61, 2011. ,
Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria, ACS Med Chem Lett, vol.2, pp.708-721, 2011. ,
Enzymes of purine and pyrimidine metabolism from the human malaria parasite, Plasmodium falciparum, Mol Biochem Parasitol, vol.5, pp.275-90, 1982. ,
Identification of broad-spectrum antiviral compounds and assessment of the druggability of their target for efficacy against respiratory syncytial virus (RSV), Proc Natl Acad Sci USA, vol.108, pp.6739-6783, 2011. ,
Broad-spectrum antiviral that interferes with de novo pyrimidine biosynthesis, Proc Natl Acad Sci USA, vol.108, pp.5777-82, 2011. ,
Original 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidine derivatives as inhibitors of human dihydroorotate dehydrogenase (DHODH), J Med Chem, vol.58, pp.860-77, 2015. ,
URL : https://hal.archives-ouvertes.fr/pasteur-01101526
Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase www.impactjournals.com/oncotarget (DHODH), J Med Chem, vol.58, pp.5579-98, 2015. ,
On dihydroorotate dehydrogenases and their inhibitors and uses, J Med Chem, vol.56, pp.3148-67, 2013. ,
URL : https://hal.archives-ouvertes.fr/pasteur-00819070
F901318 represents a novel class of antifungal drug that inhibits dihydroorotate dehydrogenase, Proc Natl Acad Sci, 2016. ,
Mechanism of action for leflunomide in rheumatoid arthritis, Clin Immunol, vol.93, pp.198-208, 1999. ,
Leflunomide: an immunomodulatory drug for the treatment of rheumatoid arthritis and other autoimmune diseases, Immunopharmacology, vol.47, pp.273-89, 2000. ,
Leflunomide in the treatment of rheumatoid arthritis, Clin Ther, vol.26, pp.90048-90051, 2004. ,
Leflunomide, a novel immunomodulator for the treatment of active rheumatoid arthritis, Clin Ther, vol.21, issue.00, pp.86732-86738, 1999. ,
Randomized trial of oral teriflunomide for relapsing multiple sclerosis, N Engl J Med, vol.365, pp.1293-303, 2011. ,
Teriflunomide for the treatment of multiple sclerosis, Clin Neurol Neurosurg, vol.115, issue.1, pp.90-94, 2013. ,
Multiple Sclerosis Oral (TEMSO) Trial Group and the MRI-AC in Houston, Texas. Long-term safety and efficacy of teriflunomide: nine-year follow-up of the randomized TEMSO study, Neurology, vol.86, pp.920-950, 2016. ,
Dihydroorotate dehydrogenase inhibitor A771726 (leflunomide) induces apoptosis and diminishes proliferation of multiple myeloma cells, Mol Cancer Ther, vol.8, pp.366-75, 2009. ,
Leflunomide reduces proliferation and induces apoptosis in neuroblastoma cells in vitro and in vivo, PLoS One, vol.8, 2013. ,
DHODH modulates transcriptional elongation in the neural crest and melanoma, Nature, vol.471, pp.518-540, 2011. ,
Pyrimidine biosynthesis links mitochondrial respiration to the p53 pathway, Proc Natl Acad Sci USA, vol.107, pp.12828-12861, 2010. ,
The Role of Dihydroorotate Dehydrogenase in Apoptosis Induction in Response to Inhibition of the Mitochondrial Respiratory Chain Complex III, Acta Naturae, vol.6, pp.69-75, 2014. ,
Inhibition of Dihydroorotate Dehydrogenase Overcomes Differentiation Blockade in Acute Myeloid Leukemia, Cell, vol.167, pp.171-186, 2016. ,
The molecular basis of mutations induced by deoxyribonucleoside triphosphate pool imbalances in mammalian cells, Exp Cell Res, vol.181, issue.89, pp.90090-90096, 1989. ,
International Commission for Protection Against Environmental Mutagens and Carcinogens. Deoxyribonucleoside triphosphate levels: a critical factor in the maintenance of genetic stability, Mutat Res, vol.318, pp.1-64, 1994. ,
Nucleotide deficiency promotes genomic instability in early stages of cancer development, Cell, vol.145, pp.435-481, 2011. ,
Dynamics of DNA replication in mammalian somatic cells: nucleotide pool modulates origin choice and interorigin spacing, Cell, vol.114, issue.03, pp.569-574, 2003. ,
DNA replication stress, genome instability and aging, Nucleic Acids Res, vol.35, pp.7545-56, 2007. ,
The chk1 pathway is required to prevent mitosis following cell-cycle arrest at 'start', Curr Biol, vol.5, pp.1179-90, 1995. ,
Activation of mammalian Chk1 during DNA replication arrest: a role for Chk1 in the intra-S phase checkpoint monitoring replication origin firing, J Cell Biol, vol.280, pp.913-936, 1998. ,
Death by releasing the breaks: CHK1 inhibitors as cancer therapeutics, Trends Mol Med, vol.17, pp.88-96, 2011. ,
The transcription factor E4F1 coordinates CHK1-dependent checkpoint and mitochondrial functions, Cell Reports, vol.11, pp.220-253, 2015. ,
URL : https://hal.archives-ouvertes.fr/hal-01213872
Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1, Mol Cancer Ther, vol.7, pp.2394-404, 2008. ,
?H2AX and Chk1 phosphorylation as predictive pharmacodynamic biomarkers of Chk1 inhibitor-chemotherapy combination treatments, BMC Cancer, vol.14, p.483, 2014. ,
CHK2 kinase in the DNA damage response and beyond, J Mol Cell Biol, vol.6, pp.442-57, 2014. ,
Australian Pancreatic Cancer Genome Initiative. Gemcitabine and CHK1 inhibition potentiate EGFR-directed radioimmunotherapy against pancreatic ductal adenocarcinoma, Clin Cancer Res, vol.20, pp.3187-97, 2014. ,
Pharmacology review(s) for Teriflunomide -Center for drug evaluation and research -Application number 202992Orig1s000, 2012. ,
Exploiting replicative stress to treat cancer, Nat Rev Drug Discov, vol.14, pp.405-428, 2015. ,
Identification of preferred chemotherapeutics for combining with a CHK1 inhibitor, Mol Cancer Ther, vol.12, pp.2285-95, 2013. ,
ATR-mediated checkpoint pathways regulate phosphorylation and activation of human Chk1, Mol Cell Biol, vol.21, pp.4129-4168, 2001. ,
CHK1 Inhibition Synergizes with Gemcitabine Initially by Destabilizing the DNA Replication Apparatus, Cancer Res, vol.75, pp.3583-95, 2015. ,
Chk1 inhibition after replicative stress activates a double strand break response mediated by ATM and DNA-dependent protein kinase, Cell Cycle, vol.9, pp.995-1004, 2010. ,
Chk1 as a new therapeutic target in triple-negative breast cancer, Breast, vol.23, pp.250-58, 2014. ,
Identification of a novel Raf-1 pathway activator that inhibits gastrointestinal carcinoid cell growth, Mol Cancer Ther, vol.9, pp.429-466, 2010. ,
Resistance to chemotherapeutic antimetabolites: a function of salvage pathway involvement and cellular response to DNA damage, Br J Cancer, vol.75, pp.935-980, 1997. ,
Spotlight on teriflunomide, Int MS J, vol.15, pp.62-68, 2008. ,
New colorimetric cytotoxicity assay for anticancer-drug screening, J Natl Cancer Inst, vol.82, pp.1107-1119, 1990. ,