Targeting schistosome histone modifying enzymes for drug development
…, F Dubois-Abdesselem, J Lancelot… - Current …, 2012 - ingentaconnect.com
The histone modifying enzymes (HME) represent particularly promising targets for the
development of alternatives to praziquantel, the only currently available drug to combat …
development of alternatives to praziquantel, the only currently available drug to combat …
[HTML][HTML] Structural Basis for the Inhibition of Histone Deacetylase 8 (HDAC8), a Key Epigenetic Player in the Blood Fluke Schistosoma mansoni
…, V Cura, DA Stolfa, K Schmidtkunz, J Lancelot… - PLoS …, 2013 - journals.plos.org
The treatment of schistosomiasis, a disease caused by blood flukes parasites of the Schistosoma
genus, depends on the intensive use of a single drug, praziquantel, which increases …
genus, depends on the intensive use of a single drug, praziquantel, which increases …
[HTML][HTML] Epigenetic control of gene function in schistosomes: a source of therapeutic targets?
A Cabezas-Cruz, J Lancelot, S Caby, G Oliveira… - Frontiers in …, 2014 - frontiersin.org
The discovery of the epigenetic regulation of gene expression has revolutionized both our
understanding of how genomes function and approaches to the therapy of numerous …
understanding of how genomes function and approaches to the therapy of numerous …
Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis
T Heimburg, A Chakrabarti, J Lancelot… - Journal of Medicinal …, 2016 - ACS Publications
Schistosomiasis is a major neglected parasitic disease that affects more than 265 million
people worldwide and for which the control strategy consists of mass treatment with the only …
people worldwide and for which the control strategy consists of mass treatment with the only …
[HTML][HTML] Effect of clinically approved HDAC inhibitors on Plasmodium, Leishmania and Schistosoma parasite growth
MJ Chua, MSJ Arnold, W Xu, J Lancelot… - International Journal for …, 2017 - Elsevier
Malaria, schistosomiasis and leishmaniases are among the most prevalent tropical parasitic
diseases and each requires new innovative treatments. Targeting essential parasite …
diseases and each requires new innovative treatments. Targeting essential parasite …
Characterization of histone deacetylase 8 (HDAC8) selective inhibition reveals specific active site structural and functional determinants
…, T Heimburg, A Chakrabarti, J Lancelot… - Journal of medicinal …, 2018 - ACS Publications
Metal-dependent histone deacetylases (HDACs) are key epigenetic regulators that represent
promising therapeutic targets for the treatment of numerous human diseases. Yet the …
promising therapeutic targets for the treatment of numerous human diseases. Yet the …
[HTML][HTML] Schistosoma mansoni Sirtuins: Characterization and Potential as Chemotherapeutic Targets
J Lancelot, S Caby, F Dubois-Abdesselem… - PLoS neglected …, 2013 - journals.plos.org
Background The chemotherapy of schistosomiasis currently depends on the use of a single
drug, praziquantel. In order to develop novel chemotherapeutic agents we are investigating …
drug, praziquantel. In order to develop novel chemotherapeutic agents we are investigating …
[HTML][HTML] Molecular basis for the antiparasitic activity of a mercaptoacetamide derivative that inhibits histone deacetylase 8 (HDAC8) from the human pathogen …
DA Stolfa, M Marek, J Lancelot, AT Hauser… - Journal of molecular …, 2014 - Elsevier
Schistosomiasis, caused by the parasitic flatworm Schistosoma mansoni and related species,
is a tropical disease that affects over 200 million people worldwide. A new approach for …
is a tropical disease that affects over 200 million people worldwide. A new approach for …
[HTML][HTML] A Novel Class of Schistosoma mansoni Histone Deacetylase 8 (HDAC8) Inhibitors Identified by Structure-Based Virtual Screening and In Vitro Testing
…, A Chakrabarti, K Schmidtkunz, M Marek, J Lancelot… - Molecules, 2018 - mdpi.com
A promising means in the search of new small molecules for the treatment of schistosomiasis
(amongst other parasitic ailments) is by targeting the parasitic epigenome. In the present …
(amongst other parasitic ailments) is by targeting the parasitic epigenome. In the present …
[HTML][HTML] Epigenetic changes modulate schistosome egg formation and are a novel target for reducing transmission of schistosomiasis
…, EJL Torres, S Caby, J Lancelot… - PLoS …, 2014 - journals.plos.org
Treatment and control of schistosomiasis relies on the only available drug, praziquantel, and
the search for alternative chemotherapeutic agents is therefore urgent. Egg production is …
the search for alternative chemotherapeutic agents is therefore urgent. Egg production is …