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Targeting Malaria Epigenetics
Ludovic Halby (PI)
Malaria is a tropical disease due to a parasite named Plasmodium. It is a global health problem, still causing more than 450.000 deaths each year (mostly African children) and over 200 million infections (http://www.who.int/malaria/en/). […]
(EN) Dr. Paola B. Arimondo works at the interface of Chemistry and Biology and develop original chemical tools able (i) to elucidate, at the molecular level, the biological mechanisms that are aberrant in human diseases and (ii) to target these mechanisms aiming at novel therapeutic strategies. She studied Chemistry at the University of Pisa (Scuola Normale Superiore, Italy) and received her Ph.D in Biophysics at the MNHN in Paris. In October 2001, Paola Arimondo was recruited by the CNRS in Paris. Her research focused on the interactions between nucleic acids and proteins and their modulation by small chemical molecules. Initially she developed a strategy to target at a specific DNA site a class of antitumor agents directed against human DNA topoisomerases I and II, resulting in site-specific “DNA scissors”. The strategy was patented and developed in collaboration with a pharmaceutical company, Sigma Tau, Italy. After a six-month sabbatical in 2005 at the University of California in Berkeley, she initiated a new project developing an innovative antitumor strategy aiming at the epigenetic control of gene expression in cancers. In 2011, Paola Arimondo was recruited to lead the Laboratory of Epigenetic Targeting of Cancer (ETaC) USR3388, a joint public-private Laboratory between the CNRS and Pierre Fabre Laboratories, in Toulouse, France. ETaC research projects spanned from the chemistry of the natural products to the discovery of chemical modulators of DNA methylation in cancer. Under her leadership the ETaC laboratory in Toulouse has discovered novel potential drugs and biomarkers. In 2016-2017 she was Oversea Fellow of the Churchill College, Cambridge, UK. In January 2018 she start a new Research Unit Epigenetic Chemical Biology (EpiChBio) at the Institut Pasteur dedicated to the design and use of novel chemical tools to study the molecular mechanisms underlying the aberrant methylation in cancer cells towards a better understanding of the disease and how to target it. The Institut Pasteur offers a unique integrated research frame from microbiology to cancer, from chemistry, structural biology to cellular biology and in vivo experiments. The chemical tools I develop will bring an alternative approach to address the biological questions and, in return, their knowledge and expertise in biology will be a certain asset for our research.
2021Targeting Germ Cell Tumors with the Newly Synthesized Flavanone-Derived Compound MLo1302 Efficiently Reduces Tumor Cell Viability and Induces Apoptosis and Cell Cycle Arrest., Pharmaceutics 2021 Jan; 13(1): .
2020Bisubstrate inhibitors: the promise of a selective and potent chemical inhibition of epigenetic ‘writers’, Epigenomics, Sep. 2020.
2020Chapter 4 – Targeting DOT1L for mixed-lineage rearranged leukemia, Histone Modifications in Therapy, Translational Epigenetics 2020.
2020Wandering along the epigenetic timeline., Clin Epigenetics 2020 07; 12(1): 97.
2020Study of the Effect of Substituents of ortho-Phenylenediamines in the Opening of Lactones and Lactams for Access to Benzimidazol-2-yl Alkanols and Benzimidazol-2-yl Alkylamines., SynLett 2020 31.
2020Bisubstrate-type chemical probes identify GRP94 as a potential target of cytosine-containing adenosine analogs, ACS Chem. Biol. 2020 Mar;.
2020Novel Quinoline Compounds Active in Cancer Cells through Coupled DNA Methyltransferase Inhibition and Degradation, Cancers (Basel) 2020 Feb;12(2).
2019The timeline of epigenetic drug discovery: from reality to dreams, Clin Epigenetics 2019 12;11(1):174.
2019DNA Methylation Bisubstrate Inhibitors Are Fast-Acting Drugs Active against Artemisinin-Resistant Parasites, ACS Cent Sci 2020 Jan;6(1):16-21.
2019Synthesis of novel 3-halo-3-nitroflavanones and their activities as DNA methyltransferase inhibitors in cancer cells, Eur J Med Chem 2020 Jan;186:111829.
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