Yves Pommier

TL;DR: A number of patented HIV-1 IN inhibitors, especially those that possess high selectivity for the strand transfer reaction, are reviewed, particularly those that have a polar coplanar moiety.

TL;DR: Rec recombinant large T antigen (T-Ag), a virus encoded helicase with strong affinity for tumor suppressors and cell cycle- and replication-related proteins, suppresses top1 cleavage complexes and top1 catalytic activity and suggests the importance of top1-protein interactions for the regulation of DNA replication and modulation of camptothecin activity.

TL;DR: It is demonstrated that, like RAL, MK-0536 is highly potent against recombinant IN and viral replication and also effective against INs that carry the three main RAL resistance mutations and against the G118R mutant.

TL;DR: The overall repair capacity estimated by the ability of cells to reactivate UV-damaged pSV-CAT plasmid was increased in MCF-7/C4 cells, suggesting that enhanced DNA repair is one of the factors involved in CPT resistance.

TL;DR: 2-position-modified indenoisoquinolines modified at the 2-position with three-carbon side chains ending with amino substituents are described as dual Top1–TDP1 inhibitors using a structure-based drug design approach.