• Publications
  • Influence
Topoisomerase I inhibitors: camptothecins and beyond
  • Y. Pommier
  • Biology, Medicine
  • Nature Reviews Cancer
  • 1 October 2006
TLDR
The mechanisms and molecular determinants of tumour response to TOP1 inhibitor are reviewed, and rational combinations of TOP1 inhibitors with other drugs are considered based on current knowledge of repair and checkpoint pathways that are associated with TOP1-mediated DNA damage. Expand
Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors.
TLDR
This study shows that PARP inhibitors trap the PARP1 and PARP2 enzymes at damaged DNA, providing a new mechanistic foundation for the rational application ofPARP inhibitors in cancer therapy. Expand
DNA topoisomerases and their poisoning by anticancer and antibacterial drugs.
TLDR
This review focuses on the molecular and biochemical characteristics of topoisomerases and their inhibitors and discusses the common mechanism of action ofTopoisomerase poisons by interfacial inhibition and trapping of topisomerase cleavage complexes. Expand
A gene expression database for the molecular pharmacology of cancer
TLDR
Gene-drug relationships for the clinical agents 5-fluorouracil and L-asparaginase exemplify how variations in the transcript levels of particular genes relate to mechanisms of drug sensitivity and resistance. Expand
γH2AX and cancer
TLDR
Using γH2AX detection to determine the extent of DSB induction may help to detect precancerous cells, to stage cancers, to monitor the effectiveness of cancer therapies and to develop novel anticancer drugs. Expand
Integrase inhibitors to treat HIV/Aids
TLDR
This review focuses on the molecular basis and rationale for developing integrase inhibitors, as well as the main classes of lead compounds and interfacial inhibitors of protein–nucleic-acid interactions that might apply to the clinically used strand-transfer inhibitors. Expand
CellMiner: a web-based suite of genomic and pharmacologic tools to explore transcript and drug patterns in the NCI-60 cell line set.
TLDR
A CellMiner web application is introduced designed to improve the use of the extensive NCI-60 cell line database for discovery by creating web-based processes that are rapid, flexible, and readily applied by users without bioinformatics expertise. Expand
Drugging topoisomerases: lessons and challenges.
  • Y. Pommier
  • Biology, Medicine
  • ACS chemical biology
  • 18 January 2013
TLDR
This review discusses how topoisomerase inhibitors kill cells by trapping topoisomersases on DNA rather than by classical enzymatic inhibition, and extends to a novel mechanism of action of PARP inhibitors and could be applied to the targeting of transcription factors. Expand
Initiation of DNA Fragmentation during Apoptosis Induces Phosphorylation of H2AX Histone at Serine 139*
TLDR
It is shown that γ-H2AX formation is an early chromatin modification following initiation of DNA fragmentation during apoptosis, and it is indicated that any apoptotic endonuclease is sufficient to induce this phosphorylated form of H2AX. Expand
Stereospecific PARP Trapping by BMN 673 and Comparison with Olaparib and Rucaparib
TLDR
BMN 673 is the most potent clinical PARP inhibitor tested to date with the highest efficiency at trapping PARP–DNA complexes and is also approximately 100-fold more cytotoxic than olaparib and rucaparIB in combination with the DNA alkylating agents methyl methane sulfonate and temozolomide. Expand
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