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Parp inhibitors

2016
Inhibition of Poly (ADP-ribose) polymerase 1 has relatively recently entered the clinic. The ground-breaking drug both scientifi cally and clinically was olaparib, but several other PARP inhibitors are in development. This treatment is the fi rst to therapeutically exploit mutant recessive cancer genes.
Grève, J.De   +8 more
openaire   +1 more source

PARP inhibitors for anticancer therapy

Biochemical Society Transactions, 2014
PARP-1 [poly(ADP-ribose) polymerase-1], which plays a key role in DNA repair, was discovered 50 years ago. PARPi (PARP inhibitors), originally made to probe the function of the enzyme, inhibit DNA repair and increase the potency of anticancer cytotoxic agents.
openaire   +3 more sources

A snapshot of chemoresistance to PARP inhibitors

Trends in Pharmacological Sciences, 2012
The exploitation of synthetic lethality in BRCA-deficient tumor carriers using potent inhibitors of the enzyme poly(ADP-ribose) polymerase (PARP)-1 has led to an enthusiastic response among basic scientists, oncologists and pharmaceutical companies. However, accumulating evidence demonstrates that resistance to these drugs develops in tumors in both ...
openaire   +3 more sources

Evolution of the Development of PARP Inhibitors

2023
PARP inhibitors first entered the clinic in 2003 in combination with DNA damaging agents in an attempt to overcome treatment resistance to established agents. A brief overview of ADP-ribosylator enzyme biology and the early preclinical development of the class is discussed, illustrating the multiple biological activities of these enzymes and potential ...
openaire   +2 more sources

Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2

European Journal of Medicinal Chemistry, 2022
Yiliang Li, Jiang Yu, Wenfeng Gou
exaly  

The forefront of ovarian cancer therapy: update on PARP inhibitors

Annals of Oncology, 2020
Isabelle Ray-Coquard   +2 more
exaly  

Poly(ADP-Ribose) polymerase (PARP) inhibitors: Exploiting a synthetic lethal strategy in the clinic†‡

Ca-A Cancer Journal for Clinicians, 2011
Johann de Bono   +2 more
exaly  

PARP Inhibitors

2014
Joaquin Mateo   +2 more
openaire   +1 more source

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