Yves Pommier

TL;DR: The curation and common annotations provided here across pharmacogenomic datasets increase the utility of the individual datasets to address multiple researcher question types, including data reproducibility, biomarker discovery and multivariate analysis of drug activity.

TL;DR: The crystal structure of human topoisomerase I in noncovalent complex with a DNA oligonucleotide containing 8-oxoG at the +1 position in the scissile strand shows the docked, inactive conformation of Tyr-723–Phe is reminiscent of the related tyrosine recombinase family of integrases and recombinases, suggesting a common regulatory mechanism.

TL;DR: The ring E modified analogues 2d-f display little or no cytotoxic activity, greatly reduced effect on the inhibition of topoisomerase I, and total loss of life prolongation in the in vivo L-1210 mouse leukemia assay, indicative of the highly restricted structural and electronic requirements of ring E for biological activity in camptothecin.

TL;DR: In this article, the cocrystal structure of PV1019 bound in the ATP binding pocket of Chk2 confirmed enzymatic/biochemical observations that PV 1019 acts as a competitive inhibitor of ChK2 with re

TL;DR: The integration reactions in the retrovirus life cycle and the integrase protein are described and a comprehensive review of the inhibitors identified to date is provided.