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PARP inhibitors

The Ubiquitin-Dependent ATPase p97 Removes Cytotoxic Trapped PARP1 from Chromatin

[Nature Cell Biology] Using wild-type and a trapping-deficient poly (ADP-ribose) polymerase (PARP1) mutant combined with rapid immunoprecipitation mass spectrometry of endogenous proteins and Apex2 proximity labeling, investigators delineated mass spectrometry-based interactomes of trapped and non-trapped PARP1.

FDI-6 Inhibits the Expression and Function of FOXM1 to Sensitize BRCA-Proficient Triple-Negative Breast Cancer Cells to Olaparib by Regulating Cell Cycle Progression and DNA...

[Cell Death & Disease] Scientists found that repression of the oncogenic transcription factor FOXM1 using FOXM1 shRNA or FOXM1 inhibitor FDI-6 could sensitize BRCA-proficient TNBC to PARP inhibitor Olaparib in vitro and in vivo.

Prognostic and Therapeutic Significance of COP9 Signalosome Subunit CSN5 in Prostate Cancer

[Oncogene] Deregulation of CSN5, a putative androgen receptor (AR), could affect diverse cellular functions that contribute to tumor development. Inhibition of CSN5 repressed metabolic pathways, including oxidative phosphorylation and glycolysis in AR-negative prostate cancer cells.

Treatment Landscape of Triple-Negative Breast Cancer — Expanded Options, Evolving Needs

[Nature Reviews Clinical Oncology] Scientists describe the current and upcoming therapeutic landscape of TNBC and discuss how an integrated view of the TNBC ecosystem can define different levels of risk and provide improved opportunities for tailoring treatment.

Rakovina Therapeutics Partners with St. Baldrick’s Foundation to Research and Develop New Treatments for Childhood Bone Cancer

[Rakovina Therapeutics, Inc.] Rakovina Therapeutics, Inc. announced that the company has been selected to join a three year US $975,000 research program funded by the St. Baldrick’s Foundation Martha’s BEST Grant for All, which is aimed at developing new treatments for Ewing sarcoma, an aggressive bone and soft tissue cancer in children and young adults.

MET Inhibition Enhances PARP Inhibitor Efficacy in Castration-Resistant Prostate Cancer by Suppressing the ATM/ATR and PI3K/AKT Pathways

[Journal of Cellular and Molecular Medicine] Researchers demonstrated that mesenchymal–epithelial transition (MET) inhibition enhanced sensitivity of CRPC to poly adenosine diphosphate–ribose polymerase (PARP) inhibitors by suppressing the ATM/ATR and phosphoinositide 3-kinase/protein kinase B (PI3K/AKT) pathways.

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