Homologous recombination proficiency in ovarian and breast cancer patients

JF Creeden, NS Nanavaty, KR Einloth, CE Gillman… - BMC cancer, 2021 - Springer
Homologous recombination and DNA repair are important for genome maintenance.
Genetic variations in essential homologous recombination genes, including BRCA1 and …

New horizons of synthetic lethality in cancer: current development and future perspectives

V Previtali, G Bagnolini, A Ciamarone… - Journal of Medicinal …, 2024 - ACS Publications
In recent years, synthetic lethality has been recognized as a solid paradigm for anticancer
therapies. The discovery of a growing number of synthetic lethal targets has led to a …

Discovery of 4-hydroxyquinazoline derivatives as small molecular BET/PARP1 inhibitors that induce defective homologous recombination and lead to synthetic …

J Zhang, C Yang, P Tang, J Chen… - Journal of Medicinal …, 2022 - ACS Publications
The effective potency and resistance of poly (ADP-ribose) polymerase (PARP) inhibitors limit
their application. Here, we exploit a new paradigm that mimics the effects of breast cancer …

New RAD51 inhibitors to target homologous recombination in human cells

IS Shkundina, AA Gall, A Dick, S Cocklin, AV Mazin - Genes, 2021 - mdpi.com
Targeting DNA repair proteins with small-molecule inhibitors became a proven anti-cancer
strategy. Previously, we identified an inhibitor of a major protein of homologous …

Recent advances in the development of non-PIKKs targeting small molecule inhibitors of DNA double-strand break repair

JM Kelm, A Samarbakhsh, A Pillai… - Frontiers in …, 2022 - frontiersin.org
The vast majority of cancer patients receive DNA-damaging drugs or ionizing radiation (IR)
during their course of treatment, yet the efficacy of these therapies is tempered by DNA …

Combining PARP inhibition with platinum, ruthenium or gold complexes for cancer therapy

NA Yusoh, H Ahmad, MR Gill - ChemMedChem, 2020 - Wiley Online Library
Platinum drugs are heavily used first‐line chemotherapeutic agents for many solid tumours
and have stimulated substantial interest in the biological activity of DNA‐binding metal …

Discovery of ruthenium (II) metallocompound and olaparib synergy for cancer combination therapy

NA Yusoh, PR Tiley, SD James, SN Harun… - Journal of Medicinal …, 2023 - ACS Publications
Synergistic drug combinations can extend the use of poly (ADP-ribose) polymerase
inhibitors (PARPi) such as Olaparib to BRCA-proficient tumors and overcome acquired or de …

Synthetic lethality in pancreatic cancer: discovery of a new RAD51-BRCA2 small molecule disruptor that inhibits homologous recombination and synergizes with …

G Bagnolini, D Milano, M Manerba… - Journal of Medicinal …, 2020 - ACS Publications
Synthetic lethality is an innovative framework for discovering novel anticancer drug
candidates. One example is the use of PARP inhibitors (PARPi) in oncology patients with …

A small-molecule inhibitor of the BRCA2-RAD51 interaction modulates RAD51 assembly and potentiates DNA damage-induced cell death

DE Scott, NJ Francis-Newton, ME Marsh, AG Coyne… - Cell chemical …, 2021 - cell.com
BRCA2 controls RAD51 recombinase during homologous DNA recombination (HDR)
through eight evolutionarily conserved BRC repeats, which individually engage RAD51 via …

Identification of RAD51–BRCA2 Inhibitors Using N-Acylhydrazone-Based Dynamic Combinatorial Chemistry

G Bagnolini, B Balboni, F Schipani… - ACS Medicinal …, 2022 - ACS Publications
RAD51 is an ATP-dependent recombinase, recruited by BRCA2 to mediate DNA double-
strand breaks repair through homologous recombination and represents an attractive cancer …