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Targeting of 5-aza-2'-deoxycytidine residues by chromatin-associated DNMT1 induces proteasomal degradation of the free enzyme.
Katan Patel, Jacqueline Dickson, Shahida Din, Kenneth Macleod, Duncan Jodrell, Bernard Ramsahoye
Sep 03, 2020
5-Aza-2'-deoxycytidine (5-aza-dC) is a nucleoside analogue with cytotoxic and DNA demethylating effects. Here we show that 5-aza-dC induces the proteasomal degradation of free (non-chromatin bound) DNMT1 through a mechanism...
Selective inactivation of hypomethylating agents by SAMHD1 provides a rationale for therapeutic stratification in AML.
Thomas Oellerich, Constanze Schneider, Dominique Thomas, Kirsten M Knecht, Olga Buzovetsky, Lars Kaderali, Christoph Schliemann, Hanibal Bohnenberger, Linus Angenendt, Wolfgang Hartmann, Eva Wardelmann, Tamara Rothenburger, Sebastian Mohr, Sebastian Scheich, Federico Comoglio, Anne Wilke, Philipp Ströbel, Hubert Serve, Martin Michaelis, Nerea Ferreirós, Gerd Geisslinger, Yong Xiong, Oliver T Keppler, Jindrich Cinatl
Aug 01, 2020
Hypomethylating agents decitabine and azacytidine are regarded as interchangeable in the treatment of acute myeloid leukemia (AML). However, their mechanisms of action remain incompletely understood, and predictive biomarkers...
Animals Antimetabolites Antineoplastic Azacitidine Biomarkers Tumor Bone Marrow Cell Line Tumor DNA Methylation Decitabine Drug Resistance Neoplasm Female Gene Expression Regulation Leukemic Humans Leukemia Myeloid Acute Mice Patient Selection Primary Cell Culture Retrospective Studies SAM Domain and HD Domain-Containing Protein 1 Treatment Outcome Xenograft Model Antitumor Assays
In vitro and in vivo activity and cross resistance profiles of novel ruthenium (II) organometallic arene complexes in human ovarian cancer.
Ruthenium complexes offer the potential of reduced toxicity, a novel mechanism of action, non-cross resistance and a different spectrum of activity compared to platinum containing compounds. Thirteen novel ruthenium(II)...
ATP Binding Cassette Transporter Subfamily B Member 1 Animals Antimetabolites Antineoplastic Antineoplastic Agents Azacitidine Calcium Channel Blockers Carboplatin cisplatin Decitabine Drug Design Drug Resistance Multiple Drug Resistance Neoplasm Drug Screening Assays Antitumor Edetic Acid Female Humans Ligands Mice Mice Nude Neoplasm Proteins Organometallic Compounds Ovarian Neoplasms Ruthenium Compounds Structure-Activity Relationship Verapamil Xenograft Model Antitumor Assays