Yves Pommier

TL;DR: Site-directed mutagenesis was used to substitute the basic amino acid of the LdTopIL subunit by the neutral amino acid alanine and these mutants were insensitive to the inhibitor; despite they displayed significant relaxation activity.

TL;DR: Indenoisoquinoline analogs have been screened in the National Cancer Institute's hollow fiber assay (HFA) and demonstrated significant activity at intraperitoneal and subcutaneous fiber placement sites, along with net cancer cell kill in one or more cell lines.

TL;DR: Interestingly, the conjugates induced specific DNA cleavage by topo I at the triplex site even when poorly active or inactive CPT derivatives were used, suggesting that the positioning of the drug in the cleavage complex by the sequence-specific DNA ligand is able to stabilize the ternary complex, even when important interactions between topo II and CPT are disrupted.

TL;DR: In this article, the effects of two epigenetic modifiers, an EZH2 inhibitor, tazemetostat (EPZ6438), and a histone deacetylase inhibitor, panobinostat, LBH589, on SLFN11 expression in Germinal center B-cells (GCBs) during B-cell development were investigated.

TL;DR: Using a compound-guided target identification approach, high topoisomerase I (Topo I) expression levels in breast CSC-like cells and primary breast C SCs are found and promote Topo I as a potential molecular therapeutic target for therapies aimed at expunging CSCs.