The CHK1 Inhibitor Prexasertib Exhibits Monotherapy Activity in High-Grade Serous Ovarian Cancer Models and Sensitizes to PARP Inhibition
Sign Up to like & getrecommendations! Published in 2019 at "Clinical Cancer Research"
DOI: 10.1158/1078-0432.ccr-19-0448
Abstract: Purpose: PARP inhibitors are approved for the treatment of high-grade serous ovarian cancers (HGSOC). Therapeutic resistance, resulting from restoration of homologous recombination (HR) repair or replication fork stabilization, is a pressing clinical problem. We assessed… read more here.
Keywords: replication; activity; monotherapy; prexasertib ... See more keywords
CHK1/2 Inhibitor Prexasertib Suppresses NOTCH Signaling and Enhances Cytotoxicity of Cisplatin and Radiation in Head and Neck Squamous Cell Carcinoma
Sign Up to like & getrecommendations! Published in 2020 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.mct-19-0946
Abstract: Platinum-based chemoradiotherapy is a mainstay of organ-preserving therapy for patients with head and neck squamous cell carcinoma cancer (HNSCC). However, the disease eventually becomes resistant to treatment necessitating new therapies. Checkpoint kinase 1 and 2… read more here.
Keywords: cisplatin radiation; notch signaling; prexasertib; cell ... See more keywords
Abstract 1562: Correlative biomarker analysis of the phase II study of prexasertib, a cell cycle checkpoint kinase 1 (CHK1) inhibitor, in BRCA wild-type (BRCAwt), platinum-resistant recurrent, high-grade serous ovarian cancer (PR-HGSOC)
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-1562
Abstract: Background: High unmet needs exist to develop novel therapeutics and identify biomarkers to predict response in PR-HGSOC. We previously reported clinical activity of CHK1 inhibitor (CHK1i), prexasertib (a.k.a.ACR-368) in heavily pretreated BRCAwt PR-HGSOC (response rate… read more here.
Keywords: cycle; brcawt; analysis; response ... See more keywords
Selectively Targeting Checkpoint Kinase By Prexasertib Had Potent Anti-Tumor Activity As Single Agent or Combined with Other Chemotherapeutic Drugs in Diffuse Large B-Cell Lymphoma, Especially Double Hit Lymphoma
Sign Up to like & getrecommendations! Published in 2018 at "Blood"
DOI: 10.1182/blood-2018-99-110282
Abstract: Background: Relapsed/Refractory diffuse large B-cell lymphoma (DLBCL) patients had a poor prognosis, especially those relapsing within 12 months of completion therapy. Clinically, there is a need to identify and target pathways associated with acquired treatment… read more here.
Keywords: lymphoma; dlbcl; prexasertib; checkpoint kinase ... See more keywords
A pan-cancer transcriptome analysis identifies replication fork and innate immunity genes as modifiers of response to the CHK1 inhibitor prexasertib
Sign Up to like & getrecommendations! Published in 2020 at "Oncotarget"
DOI: 10.18632/oncotarget.27400
Abstract: The combined influence of oncogenic drivers, genomic instability, and/or DNA damage repair deficiencies increases replication stress in cancer. Cells with high replication stress rely on the upregulation of checkpoints like those governed by CHK1 for… read more here.
Keywords: cancer; innate immunity; chk1 inhibitor; prexasertib ... See more keywords
Prexasertib increases the sensitivity of pancreatic cancer cells to gemcitabine and S‑1.
Sign Up to like & getrecommendations! Published in 2019 at "Oncology reports"
DOI: 10.3892/or.2019.7421
Abstract: Our previous study demonstrated that gemcitabine (GEM), S‑1, and a combination of GEM and S‑1 (GS) induced S‑phase arrest and increased the phosphorylation of checkpoint kinase 1 (Chk1), which is a critical mediator of cell… read more here.
Keywords: combination; pancreatic cancer; prexasertib; effect ... See more keywords