Appropriate selection of PARP inhibitors in ovarian cancer

M Smith, B Pothuri - Current Treatment Options in Oncology, 2022 - Springer
Opinion statement Poly-ADP-ribose polymerase inhibitors (PARPi) are a class of anti-cancer
drugs that target DNA repair pathways and have shown promising efficacy in patients with …

Preclinical characterization of AZD5305, a next-generation, highly selective PARP1 inhibitor and trapper

G Illuzzi, AD Staniszewska, SJ Gill, A Pike… - Clinical cancer …, 2022 - AACR
Purpose: We hypothesized that inhibition and trapping of PARP1 alone would be sufficient
to achieve antitumor activity. In particular, we aimed to achieve selectivity over PARP2 …

PARP1 as a therapeutic target in acute myeloid leukemia and myelodysplastic syndrome

CN Kontandreopoulou, PT Diamantopoulos… - Blood …, 2021 - ashpublications.org
Abstract Poly (ADP‐ribose) polymerase 1 (PARP1) is a key mediator of various forms of
DNA damage repair and plays an important role in the progression of several cancer types …

Identification of different side effects between PARP inhibitors and their polypharmacological multi‐target rationale

D Sandhu, AA Antolin, AR Cox… - British journal of clinical …, 2022 - Wiley Online Library
Aims The aim of this study was to determine the differences and potential mechanistic
rationale for observed adverse drug reactions (ADRs) between four approved PARP …

Preclinical Characterization of AZD9574, a Blood–Brain Barrier Penetrant Inhibitor of PARP1

AD Staniszewska, D Pilger, SJ Gill, K Jamal… - Clinical Cancer …, 2024 - AACR
Purpose: We evaluated the properties and activity of AZD9574, a blood–brain barrier (BBB)
penetrant selective inhibitor of PARP1, and assessed its efficacy and safety alone and in …

Two cocrystals of olaparib with flavonoids toward sustained release: structure, dissolution behavior, and anticancer activity analysis

C Duan, Y Chen, Y Zhang, F Liang, W Liu… - Crystal Growth & …, 2022 - ACS Publications
As the first FDA-approved PARP1/2 inhibitor, olaparib (OLA) is a blockbuster anticancer
drug, but its use has been limited by the dose-limiting toxicity and short half life of …

Homologous recombination deficiency (HRD) in cutaneous oncology

FA Akinjiyan, R Morecroft, J Phillipps… - International journal of …, 2023 - mdpi.com
Skin cancers, including basal cell carcinoma (BCC), cutaneous squamous cell carcinoma
(SCC), and melanoma, are the most common malignancies in the United States. Loss of …

PARP inhibitors and haematological malignancies—friend or foe?

KA Skelding, LF Lincz - Cancers, 2021 - mdpi.com
Simple Summary PARP inhibitors are a class of orally active drugs that kill a range of cancer
types by inducing synthetic lethality. The usefulness of PARP inhibitors for the treatment of …

Design of Selective PARP-1 Inhibitors and Antitumor Studies

Y Zhang, X Li, F Liu, X Bai, X Liu, H Sun… - Journal of Medicinal …, 2024 - ACS Publications
Designing selective PARP-1 inhibitors has become a new strategy for anticancer drug
development. By sequence comparison of PARP-1 and PARP-2, we identified a possible …

The current state of the art in PARP inhibitor-based delivery nanosystems

L Cai, X Xu, W Chen - Pharmaceutics, 2022 - mdpi.com
Poly (adenosine diphosphate [ADP]–ribose) polymerases inhibitors (PARPi), the first
clinically approved drug that exhibits synthetic lethality, are moving to the forefront of cancer …