Preclinical chemosensitization by PARP inhibitors

DR Shalinsky, CK Donawho, G Los… - PARP Inhibitors for Cancer …, 2015 - Springer
Preclinical research has provided a strong rationale for employing PARP inhibitors (PARPi)
as chemosensitisers in combination with cytotoxic agents, radiosensitisers in combination …

[HTML][HTML] Improved pharmacodynamic (PD) assessment of low dose PARP inhibitor PD activity for radiotherapy and chemotherapy combination trials

R de Haan, D Pluim, B van Triest… - Radiotherapy and …, 2018 - Elsevier
Background PARP inhibitors are currently evaluated in combination with radiotherapy
and/or chemotherapy. As sensitizers, PARP inhibitors are active at very low concentrations …

[HTML][HTML] The evolving landscape of predictive biomarkers of response to PARP inhibitors

A Thomas, J Murai, Y Pommier - The Journal of clinical …, 2018 - Am Soc Clin Investig
Poly (ADP-ribose) polymerase inhibitors (PARPis) are DNA-damaging agents that trap
PARP-DNA complexes and interfere with DNA replication. Three PARPis—olaparib …

Measuring cellular PARylation to gain insight in PARP/PARG-targeted drug discovery

C Pilo, M Awad, VT Baron, F Martins, J Mikolosko… - Cancer Research, 2024 - AACR
Inhibitors of poly (ADP-ribose) polymerases (PARPs) have revolutionized cancer therapy by
highlighting the potential of synthetic lethal drugs to target the DNA damage response …

Chemopotentiation by PARP inhibitors in cancer therapy

L Tentori, G Graziani - Pharmacological research, 2005 - Elsevier
Poly (ADP-ribose) polymerases (PARP) constitute a family of enzymes involved in the
regulation of many cellular processes such as DNA repair, gene transcription, cell cycle …

The novel PARP1-selective inhibitor AZD5305 has reduced hematological toxicity when compared to PARP1/2 inhibitors in pre-clinical models

SJ Gill, R Macdonald, C Pin, R Collins, E Leonard… - Cancer Research, 2021 - AACR
Current clinical poly (ADP-ribose) polymerase (PARP) inhibitors target both PARP1 and
PARP2 and they all cause clinical cytopenias with varying severity. Understanding the …

In vitro cellular profiling of AZD5305, novel PARP1-selective inhibitor and trapper

G Illuzzi, L McWilliams, K Jamal, A Galbiati, S Bentouati… - Cancer Research, 2021 - AACR
PARP inhibitors (PARPi) have demonstrated clinical efficacy in cancers with defects in the
homologous recombination repair (HRR) pathway. Recent advances in the understanding of …

Abstract P2-05-07: Pan-cancer analysis of PARP inhibition reveals a suite of biomarkers that correlate with PARP1/2 activity in breast cancer

MSJ McDermott, DF Conklin, NA O'Brien, K Chau… - Cancer Research, 2020 - AACR
The development of multiple PARP inhibitors in BRCA mutant cancers has been one of the
most successful implementations of molecularly targeted therapies in oncology. The recent …

PARP Inhibition to Enhance Response to Chemotherapy

N Takebe, M Quinn, G Gupta, AP Chen - Targeting Cell Survival Pathways …, 2019 - Elsevier
The inhibition of poly (ADP-ribose) polymerase (PARP) enzymes is a relatively new
anticancer therapeutic strategy designed to impair the ability of tumor cells to repair DNA …

The PARP inhibitor AZD2461 provides insights into the role of PARP3 inhibition for both synthetic lethality and tolerability with chemotherapy in preclinical models

S Rulten, K Caldecott - 2016 - sussex.figshare.com
The PARP inhibitor AZD2461 was developed as a next-generation agent following olaparib,
the first PARP inhibitor approved for cancer therapy. In BRCA1-deficient mouse models …