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PARP inhibitor resistance mechanisms and PARP inhibitor derived imaging probes

Expert Review of Anticancer Therapy
Poly(ADP-ribose) polymerase 1 (PARP1) inhibition has become a major target in anticancer therapy. While PARP inhibitors (PARPi) are approved for homologous recombination (HR) deficient cancers, therapeutic resistance is a challenge and PARPi are now being investigated in cancers lacking HR deficiencies.
Tony, Yu, Benjamin H, Lok
openaire   +2 more sources

PARP trapping is governed by the PARP inhibitor dissociation rate constant

Cell Chemical Biology
Poly(ADP-ribose) polymerase (PARP) inhibitors (PARPi) are a class of cancer drugs that enzymatically inhibit PARP activity at sites of DNA damage. Yet, PARPi function mainly by trapping PARP1 onto DNA with a wide range of potency among the clinically relevant inhibitors. How PARPi trap and why some are better trappers remain unknown.
Angelica A, Gopal   +4 more
openaire   +2 more sources

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 and Epigenetic Regulation

2008
In the post-genome era attention is being focused on those epigenetic modifications which modulate chromatin structure to guarantee that information present on DNA is read correctly and at the most appropriate time in order to meet cellular requirements.
openaire   +2 more sources

Understanding and overcoming resistance to PARP inhibitors in cancer therapy

Nature Reviews Clinical Oncology, 2021
Mariana Paes Dias   +2 more
exaly  

PARPs pick-up

Nature Reviews Drug Discovery, 2016
openaire   +2 more sources

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

Ca-A Cancer Journal for Clinicians, 2011
Timothy A Yap, Johann Sebastian de Bono
exaly  

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