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PARP inhibitor resistance mechanisms and PARP inhibitor derived imaging probes
Expert Review of Anticancer TherapyPoly(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
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PARP trapping is governed by the PARP inhibitor dissociation rate constant
Cell Chemical BiologyPoly(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
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
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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
2008In 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, 2021Mariana Paes Dias +2 more
exaly
Poly(ADP-Ribose) polymerase (PARP) inhibitors: Exploiting a synthetic lethal strategy in the clinic
Ca-A Cancer Journal for Clinicians, 2011Timothy A Yap, Johann Sebastian de Bono
exaly

