Results 41 to 50 of about 1,458 (171)

Ricolinostat enhances adavosertib‑induced mitotic catastrophe in TP53‑mutated head and neck squamous cell carcinoma cells

International Journal of Oncology, 2022
TP53 mutation is one of the most frequent gene mutations in head and neck squamous cell carcinoma (HNSCC) and could be a potential therapeutic target. Recently, the WEE1 G2 checkpoint kinase (WEE1) inhibitor adavosertib (Adv) has attracted attention because of its selective cytotoxicity against TP53‑mutated cells and has shown promising activity in ...
Miyake, Keitaro, Takano, Naoharu, Kazama, Hiromi, Kikuchi, Hiroyuki, Hiramoto, Masaki, Tsukahara, Kiyoaki, Miyazawa, Keisuke   +6 more
openaire   +2 more sources

Multimetric synergy analysis of WEE1 inhibitor adavosertib with DNA-damaging drugs identifies candidate therapeutic windows in a triple-negative breast cancer cell line model

ASPET Discovery
Triple-negative breast cancer (TNBC) lacks targetable receptors and relies on the WEE1 kinase-mediated G2/M checkpoint for survival, positioning WEE1 inhibition as a rational strategy to sensitize TNBC to DNA-damaging treatments (DNAdts).
Nicole M. Nieves Avilés, Walter I. Silva Ortiz, Iris K. Salgado-Villanueva, Jing Tang, Gabriel O. Rodríguez-Vázquez, Adriana O. Díaz-Quiñones, Héctor M. Maldonado   +6 more
doaj   +1 more source

Impaired DNA double-strand break repair and effective radiosensitization of HPV-negative HNSCC cell lines through combined inhibition of PARP and Wee1

Clinical and Translational Radiation Oncology, 2023
Objectives: In head and neck squamous cell carcinoma (HNSCC), tumors negative for Human Papillomavirus (HPV) remain a difficult to treat entity and the morbidity of current multimodal treatment is high.
Agnes Oetting, Sabrina Christiansen, Fruzsina Gatzemeier, Sabrina Köcher, Lara Bußmann, Arne Böttcher, Katharina Stölzel, Anna Sophie Hoffmann, Nina Struve, Malte Kriegs, Cordula Petersen, Christian Betz, Kai Rothkamm, Henrike Barbara Zech, Thorsten Rieckmann   +14 more
doaj   +1 more source

WEE1 Inhibition in Combination With Targeted Agents and Standard Chemotherapy in Preclinical Models of Pancreatic Ductal Adenocarcinoma

Frontiers in Oncology, 2021
Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal cancer with high incidences of p53 mutations. AZD1775 (adavosertib, previously MK-1775) is a small molecule WEE1 inhibitor that abrogates the G2M checkpoint and can potentially synergize with DNA
Sarah J. Hartman, Stacey M. Bagby, Betelehem W. Yacob, Dennis M. Simmons, Morgan MacBeth, Christopher H. Lieu, S. Lindsey Davis, Alexis D. Leal, John J. Tentler, Jennifer R. Diamond, S. Gail Eckhardt, Wells A. Messersmith, Todd M. Pitts   +12 more
doaj   +1 more source

Further Understanding of High-Grade Serous Ovarian Carcinogenesis: Potential Therapeutic Targets

Cancer Management and Research, 2020
Ioannis A Voutsadakis1,2 1Algoma District Cancer Program, Sault Area Hospital, Sault Ste. Marie, Ontario, Canada; 2Section of Internal Medicine, Division of Clinical Sciences, Northern Ontario School of Medicine, Sudbury, Ontario, CanadaCorrespondence ...
Voutsadakis IA
doaj  

Dual Inhibition of PARP and the Intra-S/G2 Cell Cycle Checkpoints Results in Highly Effective Radiosensitization of HPV-Positive HNSCC Cells

Frontiers in Oncology, 2021
In head and neck squamous cell carcinoma (HNSCC), tumors positive for human papillomavirus (HPV) represent a distinct biological entity with favorable prognosis.
Katharina Hintelmann, Katharina Hintelmann, Thomas Berenz, Thomas Berenz, Malte Kriegs, Sabrina Christiansen, Sabrina Christiansen, Fruzsina Gatzemeier, Fruzsina Gatzemeier, Nina Struve, Nina Struve, Cordula Petersen, Christian Betz, Kai Rothkamm, Agnes Oetting, Agnes Oetting, Thorsten Rieckmann, Thorsten Rieckmann   +17 more
doaj   +1 more source

Translating whole‐genome doubling into precision medicine in cancer

Molecular Oncology, Volume 20, Issue 10, Page 2490-2509, October 2026.
Whole‐genome doubling creates a WGD‐positive tumor state characterized by persistent chromosomal instability, karyotypic diversification, and cellular stress. These same biological pressures drive aggressive tumor evolution while exposing therapeutic vulnerabilities, providing a rationale for WGD‐informed precision medicine. Whole‐genome doubling (WGD)
Sejung Lee, Junghyeok Lim, Jinhyuk Bhin
wiley   +1 more source

A Phase II Trial of the WEE1 Inhibitor Adavosertib in SETD2-Altered Advanced Solid Tumor Malignancies (NCI 10170) [PDF]

We sought to evaluate the efficacy of WEE1 inhibitor adavosertib in patients with solid tumor malignancies (cohort A) and clear cell renal cell carcinoma (ccRCC; cohort B). NCT03284385 was a parallel cohort, Simon two-stage, phase II study of adavosertib
Trikalinos, Nikolaos A, Kalebasty, Arash R, Boerner, Scott A, Rathmell, W Kimryn, Krings, Gregor, Bergsland, Emily K, Parikh, Mamta, LoRusso, Patricia, Balido, Celene, Burns, Timothy F, Takebe, Naoko, Aggarwal, Rahul R, Shapiro, Geoffrey I, Munster, Pamela N, Rodon, Jordi, Maldonado, Edward, Mahalingam, Devalingam, Ashworth, Alan, Burns, Timothy F., et al.,, Trikalinos, Nikolaos A., Munster, Pamela N., Boerner, Scott A., Bergsland, Emily K., Kalebasty, Arash R., Aggarwal, Rahul R., Shapiro, Geoffrey I., Rathmell, W. Kimryn   +27 more
core   +3 more sources

Supplementary Data from Safety, Antitumor Activity, and Biomarker Analysis in a Phase I Trial of the Once-daily Wee1 Inhibitor Adavosertib (AZD1775) in Patients with Advanced Solid Tumors

, 2021
Supplementary Methods, Supplementary Fig. S1 (Mean adavosertib plasma concentrations for QD vs. BID schedules), Supplementary Fig. S2 (Example PD biomarker immunofluorescence images), Supplementary Fig.
Naoko Takebe (14953338), Li Chen (5749), Abdul Rafeh Naqash (15035066), Ganesh Mugundu (10218113), Biswajit Das (15035081), Jennifer Zlott (15035075), Shivaani Kummar (107740), Ralph E. Parchment (14905824), James H. Doroshow (13270697), Deborah Wilsker (6586), Ashley Bruns (15035072), Robert J. Kinders (10881100), Larry Rubinstein (15035078), Jiuping Ji (107729), Khanh Do (1476472), Howard Streicher (3467351), Alice P. Chen (14943433), Arjun Mittra (310881), Richard Piekarz (15035022), Elad Sharon (15021041), Lamin Juwara (11100085), Ting-Chia Chang (6532961), Geraldine O'Sullivan Coyne (15035069), Sarah B. Miller (14932767)   +23 more
core   +1 more source

Introduction to Single‐Cell Physiologically‐Based Pharmacokinetic (scPBPK) Models

CPT: Pharmacometrics &Systems Pharmacology, Volume 15, Issue 9, September 2026.
ABSTRACT The current investigation introduces single‐cell physiologically based pharmacokinetic (scPBPK) models to gain insight into drug disposition at the cellular scale. The transition from standard PBPK (sPBPK) models to scPBPK models required depiction of expression‐dependent (ED) processes, such as drug metabolism or membrane transport.
Anshul Saini, James M. Gallo
wiley   +1 more source