Search Results - "Halby, Ludovic"
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triple helix: 50 years later, the outcome
Published in Nucleic acids research (01-09-2008)“…Triplex-forming oligonucleotides constitute an interesting DNA sequence-specific tool that can be used to target cleaving or cross-linking agents,…”
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2
DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge
Published in Biomolecules (Basel, Switzerland) (05-01-2017)“…Chromatin can adopt a decondensed state linked to gene transcription (euchromatin) and a condensed state linked to transcriptional repression…”
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Synthesis and Biological Activity of a Cytostatic Inhibitor of MLLr Leukemia Targeting the DOT1L Protein
Published in Molecules (Basel, Switzerland) (31-08-2021)“…Histone methyltransferase DOT1L catalyzes mono-, di- and trimethylation of histone 3 at lysine residue 79 (H3K79) and hypermethylation of H3K79 has been linked…”
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Hijacking DNA methyltransferase transition state analogues to produce chemical scaffolds for PRMT inhibitors
Published in Philosophical transactions of the Royal Society of London. Series B. Biological sciences (05-06-2018)“…DNA, RNA and histone methylation is implicated in various human diseases such as cancer or viral infections, playing a major role in cell process regulation,…”
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Direct Synthesis of Allyl Amines with 2‐Nitrosulfonamide Derivatives via the Tsuji‐Trost Reaction
Published in ChemistryOpen (Weinheim) (01-12-2021)“…The Tsuji‐Trost Reaction is a palladium‐catalysed allylation of nucleophiles that consists in the reaction of a nitrogen, carbon or oxygen‐based nucleophiles…”
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DNA Methylation Bisubstrate Inhibitors Are Fast-Acting Drugs Active against Artemisinin-Resistant Plasmodium falciparum Parasites
Published in ACS central science (22-01-2020)“…Malaria is the deadliest parasitic disease affecting over 200 million people worldwide. The increasing number of treatment failures due to multi-drug-resistant…”
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Hemisynthetic alkaloids derived from trilobine are antimalarials with sustained activity in multidrug-resistant Plasmodium falciparum
Published in iScience (17-02-2023)“…Malaria eradication requires the development of new drugs to combat drug-resistant parasites. We identified bisbenzylisoquinoline alkaloids isolated from…”
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Sequence-specific targeting of IGF-I and IGF-IR genes by camptothecins
Published in The FASEB journal (01-07-2010)“…We and others have clearly demonstrated that a topoisomerase I (Top1) inhibitor, such as camptothecin (CPT), coupled to a triplex-forming oligonucleotide (TFO)…”
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Optimized Synthesis and Enhanced Efficacy of Novel Triplex-Forming Camptothecin Derivatives Based on Gimatecan
Published in Bioconjugate chemistry (15-04-2009)“…Sequence-specific camptothecins are useful tools to inhibit specifically gene expression. The camptothecins are attached to the 3′ end of triplex-forming…”
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Targeting MDR1 gene: synthesis and cellular study of modified daunomycin-triplex-forming oligonucleotide conjugates able to inhibit gene expression in resistant cell lines
Published in Molecular pharmacology (01-05-2008)“…Reversal of the multidrug-resistant (MDR) phenotype is very important for chemotherapy success. In fact, the expression of the MDR1 gene-encoded P-glycoprotein…”
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Exploring the Cellular Activity of Camptothecin-Triple-Helix-Forming Oligonucleotide Conjugates
Published in Molecular and Cellular Biology (01-01-2006)“…Article Usage Stats Services MCB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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12
Targeting DNA Methylation with Small Molecules: What’s Next?: Miniperspective
Published in Journal of medicinal chemistry (26-03-2015)“…DNA methylation is a mammalian epigenetic mark that is involved in defining where and when genes are expressed, both in normal cells and in the context of…”
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13
Targeting DNA methylation with small molecules: what's next?
Published in Journal of medicinal chemistry (26-03-2015)“…DNA methylation is a mammalian epigenetic mark that is involved in defining where and when genes are expressed, both in normal cells and in the context of…”
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Bisubstrate inhibitors: the promise of a selective and potent chemical inhibition of epigenetic ‘writers’
Published in Epigenomics (01-09-2020)Get full text
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Editorial : Bisubstrate inhibitors: the promise of a selective and potent chemical inhibition of epigenetic “writers
Published in Epigenomics (01-09-2020)Get full text
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Towards the sustainable discovery and development of new antibiotics
Published in Nature reviews. Chemistry (2021)“…An ever-increasing demand for novel antimicrobials to treat life-threatening infections caused by the global spread of multidrug-resistant bacterial pathogens…”
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DNA methylation inhibitors in cancer: Recent and future approaches
Published in Biochimie (01-11-2012)“…This review presents the different human DNA methyltransferases (DNMTs), their biological roles, their mechanisms of action and their role in cancer. The…”
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Procainamide–SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites
Published in Journal of medicinal chemistry (22-07-2021)“…Epigenetic post-translational modifications are essential for human malaria parasite survival and progression through its life cycle. Here, we present new…”
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Rational Design of Bisubstrate-Type Analogues as Inhibitors of DNA Methyltransferases in Cancer Cells
Published in Journal of medicinal chemistry (08-06-2017)“…Aberrant DNA hypermethylation of promoter of tumor suppressor genes is commonly observed in cancer, and its inhibition by small molecules is promising for…”
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Regioselective and efficient halogenation of 4,5-unsubstituted alkyl 3-hydroxypyrrole/3-hydroxythiophene-2-yl-carboxylates
Published in Tetrahedron letters (28-06-2017)“…Substituted heterocycles, such as pyrrole and thiophene, are commonly found in the field of pharmaceutical and material sciences. Here we studied the…”
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