LOPEZ Marie
Fonction : Chargée de recherche CNRS
Thème de Recherche: Synthèse Glycosidique et Reconnaissance Moléculaire
marie.lopez
cnrs.fr
0448792142
Bureau: N3H13, Etg: 3 - Site : Pôle Chimie Balard Recherche
Activités de Recherche: |
My research aims at:
1/ identifying new strategies to target epigenetic mechanisms in pathological contexts. We are particularly interested in DNA methylation and histone acetylation and methylation that are known to cross-talk in pathological contexts. Beyond single inhibitors, we also develop hybrid inhibitors, multivalent ligands and ProTaCs and study these compounds in the context of anticancer, anti-infectious and anti-obesity treatments.
2/ designing and synthesising chemical probes to use Chemical Biology approaches to better understand epigenetic processes in cells. We developed well-design chemical probes with or without photoreactive moiety and apply them to identify molecules targets and/or location and to decipher protein networks in living systems. |
Domaines de Recherche: - Chimie/Chimie thérapeutique
- Sciences du Vivant/Cancer
- Chimie/Chimie organique
- Sciences du Vivant/Biochimie, Biologie Moléculaire/Biochimie
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Productions scientifiques :
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Targeting Germ Cell Tumors with the Newly Synthesized Flavanone-Derived Compound MLo1302 Efficiently Reduces Tumor Cell Viability and Induces Apoptosis and Cell Cycle Arrest.
Auteur(s): Lobo João, Cardoso Ana rita, Miranda-gonçalves Vera, Looijenga Leendert h j, Lopez M., Arimondo Paola b, Henrique Rui, Jerónimo Carmen
(Article) Publié:
Pharmaceutics, vol. 13 p.https://www.ncbi.nlm.nih.gov/pubmed/33430420 (2021)
PMID 33430420
DOI: 10.3390/pharmaceutics13010073
Résumé: Less toxic treatment strategies for testicular germ cell tumor (TGCT) patients are needed, as overtreatment is a concern due to the long-term side effects of platin-based chemotherapy. Although clinical benefit from classical hypomethylating agents has to date been limited, TGCTs show an abnormal DNA methylome indicating the potential of treating TGCTs with hypomethylating drugs. We tested, for the first time in TGCT cell lines, a new synthetic flavonoid compound (MLo1302) from the 3-nitroflavanone family of DNA methyltransferase (DNMT) inhibitors. We show that MLo1302 reduces cell viability (including of cisplatin resistant cell line NCCIT-R), with IC
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Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors.
Auteur(s): Morris Jason C, Chiche Johanna, Grellier Caroline, Lopez M., Bornaghi Laurent F, Maresca Alfonso, Supuran Claudiu T, Pouysségur Jacques, Poulsen Sally-Ann
(Article) Publié:
European Journal Of Medicinal Chemistry, vol. 54 p.6905-18 (2011)
Ref HAL: hal-00756639_v1
PMID 21851094
DOI: 10.1021/jm200892s
Résumé: Carbonic anhydrase (CA) enzymes, specifically membrane-bound isozymes CA IX and CA XII, underpin a pH-regulating system that enables hypoxic tumor cell survival and proliferation. CA IX and XII are implicated as potential targets for the development of new hypoxic cancer therapies. To date, only a few small molecules have been characterized in CA-relevant cell and animal model systems. In this paper, we describe the development of a new class of carbohydrate-based small molecule CA inhibitors, many of which inhibit CA IX and XII within a narrow range of low nanomolar K(i) values (5.3-11.2 nM). We evaluate for the first time carbohydrate-based CA inhibitors in cell-based models that emulate the protective role of CA IX in an acidic tumor microenvironment. Our findings identified two inhibitors (compounds 5 and 17) that block CA IX-induced survival and have potential for development as in vivo cancer cell selective inhibitors.
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Synthesis of N-Propargyl Iminosugar Scaffolds for Compound Library Generation using Click Chemistry
Auteur(s): Wilkinson Brendan, Bornaghi Laurent F, Lopez M., Healy Peter, Poulsen Sally-Ann, Houston Todd
(Article) Publié:
Australian Journal Of Chemistry, vol. 63 p.821 (2010)
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