Yves Pommier

TL;DR: It is demonstrated that this drug efficiently stabilizes topoisomerase I covalent complexes, indicating that aclacinomycin A represents a novel class of combined topoisomersase I/II inhibitor.

TL;DR: Nitrated analogues were synthesized with the inden one ring substituted with methoxy groups to further explore a previously identified structure-activity relationship between the nitrated isoquinoline ring and a methylenedioxy-substituted indenone ring and indicate that a single methoxy group at the 9-position of an indenoisoquinoline affords superior biological activity.

TL;DR: In this article, the authors further examined the sequence selectivity of camptothecin in mammalian topoisomerase I cDNA from human and Chinese hamster, and found that almost all the bases at the 3'-terminus of cleavage sites are T for calf thymus and wheat germ top iso-mase I.

TL;DR: The "drug-stacking" model proposes that topoisomerase inhibitors bind, possibly through hydrogen bonding and/or stacking, with one of the bases flanking the DNA termini and within the enzyme catalytic pocket, most likely by stacking with the catalytic tyrosine.

TL;DR: Simulation studies showed that the same core subsystem can exhibit switch-like responses both to oxygen level and to HIFalpha synthesis rate, thus suggesting a mechanism for hypoxia response promoter element-dependent responses common to both Hypoxia and growth factor signaling.