Are you sure you are not the author of this publication?
Hélène Losson Gajulapalli, Sruthi Reddy Manon Lernoux Lee, Jin-Young Mazumder, Aloran Gérard, Déborah Seidel Carole Hahn, Hyunggu Christov, Christo Dicato, Mario
...
Published in
Pharmacological Research
Despite the discovery of tyrosine kinase inhibitors (TKIs) for the treatment of breakpoint cluster region-Abelson (BCR-ABL) + cancer types, patients with chronic myeloid leukemia (CML) treated with TKIs develop resistance and severe adverse effects. Combination treatment, especially with a histone deacetylase (HDAC) 6 inhibitor (HDAC6i), appears to...
Are you sure you are not the author of this publication?
Manon Lernoux Michael Schnekenburger Hélène Losson Vermeulen, Koen Hahn, Hyunggu Gérard, Déborah Lee, Jin-Young Mazumder, Aloran Ahamed, Muneer Christov, Christo
...
Published in
Clinical Epigenetics
Background: Chronic myeloid leukemia (CML) pathogenesis is mainly driven by the oncogenic breakpoint cluster region-Abelson murine leukemia viral oncogene homolog 1 (BCR-ABL) fusion protein. Since BCR-ABL displays abnormal constitutive tyrosine kinase activity, therapies using tyrosine kinase inhibitors (TKis) such as imatinib represent a major bre...
Are you sure you are not the author of this publication?
Michael Schnekenburger Goffin, Eric Lee, Jin-Young Young Jang, Jun Mazumder, Aloran Ji, Seungwon Rogister, Bernard Bouider, Nafila Lefranc, Florence Miklos, Walter
...
Published in
Journal of Medicinal Chemistry
A new series of N-aryl-N'-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)ureas bearing an alkoxycarbonylamino group at the 6-position were synthesized and examined as putative anticancer agents targeting sirtuins in glioma cells. Based on computational docking combined to in vitro sirtuin 1/2 inhibition assays, we selected compound 18 [R/S-N-3-cyano...
Are you sure you are not the author of this publication?
Hélène Losson Michael Schnekenburger Dicato, Mario Marc Diederich
Published in
Molecules
The remarkable complexity of cancer involving multiple mechanisms of action and specific organs led researchers Hanahan and Weinberg to distinguish biological capabilities acquired by cancer cells during the multistep development of human tumors to simplify its understanding. These characteristic hallmarks include the abilities to sustain prolifera...
Are you sure you are not the author of this publication?
Cristina Florean Michael Schnekenburger Jin-Young Lee Kyung Kim Aloran Mazumder Sungmi Song Jae-Myun Kim Cindy Grandjenette Jeoung-Gyun Kim Ah-Young Yoon
...
Published in
Oncotarget
We characterized the brominated alkaloid Isofistularin-3 (Iso-3), from the marine sponge Aplysina aerophoba, as a new DNA methyltransferase (DNMT)1 inhibitor. Docking analysis confirmed our in vitro DNMT inhibition data and revealed binding of Iso-3 within the DNA binding site of DNMT1. Subsequent increased expression of tumor suppressor gene aryl ...
Are you sure you are not the author of this publication?
Seidel, Carole Marc Diederich Mazumder, Aloran Kirsch, Gilbert Dicato, Mario Michael Schnekenburger Marie-Hélène Teiten
Published in
Biochemical Pharmacology
Histone deacetylase (HDAC)6 is a unique isoenzyme targeting specific substrates including α-tubulin and heat shock protein (HSP)90. HDAC6 is involved in protein trafficking and degradation, cell shape and migration. Deregulation of HDAC6 activity is associated with a variety of diseases including cancer leading to a growing interest for developing ...
Are you sure you are not the author of this publication?
Michael Schnekenburger Marc Diederich
Published in
Current Topics in Medicinal Chemistry
A majority of cancers display alterations in epigenetic mechanisms, such as aberrant DNA methylation at CpG islands (CGIs). This local hypermethy-lation of CGIs is associated with gene silencing leading to loss of tumor sup-pressor gene (TSG) functions that are critical for the control of tumor devel-opment. Concomitantly, global genomic hypomethyl...
Are you sure you are not the author of this publication?
Miglena Koprinarova Michael Schnekenburger Marc Diederich
Published in
Current Topics in Medicinal Chemistry
Core histone acetylation is a key prerequisite for chromatin decondensation and plays a pivotal role in regulation of chromatin structure, function and dynamics. The addition of acetyl groups disturbs histone/DNA interactions in the nucleosome and alters histone/histone interactions in the same or adjacent nucleosomes. Acetyl groups can also provid...
Are you sure you are not the author of this publication?
Michael Schnekenburger Cristina Florean Dicato, Mario Marc Diederich
Published in
Current Topics in Medicinal Chemistry
Despite considerable scientific progress, the burden of cancer in our society remains a major public health problem. Tumorigenesis is recognized as a complex and multistep process that involves the accumulation of successive transformational events with multi-factorial etiology. Nevertheless, such events result in the acquisition of key hallmark ch...
Are you sure you are not the author of this publication?
Michael Schnekenburger Cristina Florean Cindy Grandjenette Marc Diederich
Published in
Current Topics in Medicinal Chemistry
Are you sure you are not the author of this publication?
Cindy Grandjenette Michael Schnekenburger Franck Morceau Mack, Fabienne Wiechmann, Katja Werz, Oliver Dicato, Mario Marc Diederich
Published in
Anti-Cancer Agents in Medicinal Chemistry
Despite recent advances in the treatment of chronic myelogenous leukemia (CML), the development of drug resistance and minimal residual disease remain major challenges for the treatment of CML patients, thus highlighting the need to develop innovative new approaches to improve therapeutic outcome. Myrtucommulone A (MCA) is a nonprenylated acylphlor...
Are you sure you are not the author of this publication?
Seidel, Carole Michael Schnekenburger Dicato, Mario Marc Diederich
Published in
Epigenomics
Histone deacetylase (HDAC)6 is a member of the class IIb HDAC family. This enzyme is zinc-dependent and mainly localized in the cytoplasm. HDAC6 is a unique isoenzyme with two functional catalytic domains and specific physiological roles. Indeed, HDAC6 deacetylates various substrates including α-tubulin and HSP90α, and is involved in protein traffi...
Are you sure you are not the author of this publication?
Michael Schnekenburger Dicato, Mario Marc Diederich
Published in
Biotechnology Advances
Carcinogenesis is a complex and multistep process that involves the accumulation of successive transformational events driven by genetic mutations and epigenetic alterations that affect major cellular processes and pathways such as proliferation, differentiation, invasion and survival. Massive deregulation of all components of the epigenetic machin...
Are you sure you are not the author of this publication?
Trécul, Anne Franck Morceau Anthoula Gaigneaux Michael Schnekenburger Dicato, Mario Marc Diederich
Published in
Biochemical Pharmacology
Valproic acid (VPA) exhibits important pharmacological properties but has been reported to trigger side effects, notably on the hematological system. We previously reported that VPA affects hematopoietic homeostasis by inhibiting erythroid differentiation and promoting myeloid and megakaryocyte differentiation. Here, we analyzed the effect of VPA o...
Are you sure you are not the author of this publication?
Seidel, Carole Michael Schnekenburger Zwergel, Clemens Francois Gaascht Mai, Antonello Dicato, Mario Kirsch, Gilbert Valente, Sergio Marc Diederich
Published in
Bioorganic & Medicinal Chemistry Letters
Histone deacetylases (HDACs) are well-established, promising targets for anticancer therapy due to their critical role in cancer development. Accordingly, an increasing number of HDAC inhibitors displaying cytotoxic effects against cancer cells have been reported. Among them, a large panel of chemical structures was described including coumarin-con...
Are you sure you are not the author of this publication?
Michael Schnekenburger Karius, Tommy Marc Diederich
Published in
Frontiers in Pharmacology
Glutathione S-transferases (GSTs) are phase II drug detoxifying enzymes that play an essential role in the maintenance of cell integrity and protection against DNA damage by catalyzing the conjugation of glutathione to a wide variety of exo- and endogenous electrophilic substrates. Glutathione S-transferase P1 (GSTP1), the gene encoding the pi-clas...
Are you sure you are not the author of this publication?
Cindy Grandjenette Michael Schnekenburger Karius, Tommy Ghelfi, Jenny Anthoula Gaigneaux Henry, Estelle Dicato, Mario Marc Diederich
Increased proliferation rates as well as resistance to apoptosis are considered major obstacles for the treatment of patients with chronic myelogenous leukemia (CML), thus highlighting the need for novel therapeutic approaches. Since senescence has been recognized as a physiological barrier against tumorigenesis, senescence-based therapy could repr...
Are you sure you are not the author of this publication?
Talhi, Oualid Michael Schnekenburger Panning, Jana G.C. Pinto, Diana Fernandes, José A. Almeida Paz, Filipe A. Jacob, Claus Marc Diederich M.S. Silva, Artur
Published in
Bioorganic & Medicinal Chemistry
Synthesis of the bis-4-hydroxycoumarin-type compound, 3,3'-[3-(2-hydroxyphenyl)-3-oxopropane-1,1-diyl]bis(4-hydroxy-2H-chromen-2-one), was performed by two alternative pathways, either involving a basic organocatalyzed 1,4-conjugate addition tandem reaction of 4-hydroxycoumarin on chromone-3-carboxylic acid, or a double condensation of 4-hydroxycou...
Are you sure you are not the author of this publication?
Rotili, Dante Tarantino, Domenico Marrocco, Biagina Gros, Christina Masson, Véronique Poughon, Valérie Ausseil, Fréderic Chang, Yanqi Labella, Donatella Cosconati, Sandro
...
Published in
PLoS ONE
Chemical manipulations performed on the histone H3 lysine 9 methyltransferases (G9a/GLP) inhibitor BIX-01294 afforded novel desmethoxyquinazolines able to inhibit the DNA methyltransferase DNMT3A at low micromolar levels without any significant inhibition of DNMT1 and G9a. In KG-1 cells such compounds, when tested at sub-toxic doses, induced the lu...
Are you sure you are not the author of this publication?
Valente, Sergio Liu, Yiwei Michael Schnekenburger Zwergel, Clemens Cosconati, Sandro Gros, Christina Tardugno, Maria Labella, Donatella Cristina Florean Minden, Steven
...
Published in
Journal of Medicinal Chemistry
DNA methyltransferases (DNMTs) are important enzymes involved in epigenetic control of gene expression and represent valuable targets in cancer chemotherapy. A number of nucleoside DNMT inhibitors (DNMTi) have been studied in cancer, including in cancer stem cells, and two of them (azacytidine and decitabine) have been approved for treatment of mye...