Results 151 to 160 of about 1,652 (181)
Phase 0 Trial of AZD1775 in First-Recurrence Glioblastoma Patients [PDF]
Clinical Cancer Research, 2018 Abstract Purpose: AZD1775 is a first-in-class Wee1 inhibitor with dual function as a DNA damage sensitizer and cytotoxic agent. A phase I study of AZD1775 for solid tumors suggested activity against brain tumors, but a preclinical study indicated minimal blood–brain barrier penetration in mice. To resolve this controversy, we examined
Nader Sanai +2 more
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AZD1775 Increases Sensitivity to Olaparib and Gemcitabine in Cancer Cells With p53 Mutations [PDF]
Cancers, 2018 Tumor suppressor p53 is responsible for enforcing cell cycle checkpoints at G1/S and G2/M in response to DNA damage, thereby allowing both normal and tumor cells to repair DNA before entering S and M. However, tumor cells with absent or mutated p53 are able to activate alternative signaling pathways that maintain the G2/M checkpoint, which becomes ...
Yujun Li +2 more
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Cancer Letters, 2020 Although trastuzumab has greatly improved the outcome of HER2-positive breast cancer, the emergence of resistance hampers its clinical benefits. Trastuzumab resistance is a multi-factorial consequence predominantly due to presence of cancer stem-like ...
Chaoyang Sun, Richard A Rovin
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Strategic Development of AZD1775, a Wee1 Kinase Inhibitor, for Cancer Therapy
Expert Opinion on Investigational Drugs, 2018Wee1 kinase controls the G2-M checkpoint. Wee1 inhibition by AZD1775 allows cells with a deregulated G1 checkpoint to progress, resulting in catastrophe and apoptosis. The challenges ahead are in the establishment of the optimum dosing schedule either alone or in combination and the identification of patients with specific biomarker profiles who ...
Funda Meric-Bernstam +2 more
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AZD1775 Plus Chemoradiotherapy for Pancreatic Cancer
Lancet Oncology, The, 2019Talha Khan Bürki
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Cancer, 2023 AbstractBackgroundInhibition of the WEE1 kinase by adavosertib (AZD1775) potentiates replicative stress from genomic instability or chemotherapy. This study reports the pediatric solid tumor phase 2 results of the ADVL1312 trial combining irinotecan and adavosertib.MethodsPediatric patients with recurrent neuroblastoma (part B), medulloblastoma/central
Kristina A Cole
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Dual Targeting of WEE1 and PLK1 by AZD1775 Elicits Single Agent Cellular Anticancer Activity [PDF]
ACS Chemical Biology, 2017 Inhibition of the WEE1 tyrosine kinase enhances anticancer chemotherapy efficacy. Accordingly, the WEE1 inhibitor AZD1775 (previously MK-1775) is currently under evaluation in clinical trials for cancer in combination with chemotherapy. AZD1775 has been reported to display high selectivity and is therefore used in many studies as a probe to interrogate
Volha Golubeva +2 more
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AZD1775 Synergizes With SLC7A11 Inhibition to Promote Ferroptosis
Science China Life SciencesTumor suppressor p53-mediated cell cycle arrest and DNA damage repair may exert cytoprotective effects against cancer therapies, including WEE1 inhibition. Considering that p53 activation can also lead to multiple types of cell death, the role of this tumor suppressor in WEE1 inhibitor-based therapies remains disputed.
Ling Hong, Qian Hao, Yingdan Huang
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Clinical Cancer Research, 2017 Purpose: AZD1775, a first-in-class, small-molecule inhibitor of the Wee1 tyrosine kinase, is under evaluation as a potential chemo- and radiosensitizer for treating glioblastoma.
Nader Sanai +2 more
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A phase II trial of the Wee1 inhibitor adavosertib (AZD1775) in recurrent uterine serous carcinoma
Gynecologic Oncology, 20206009 Background: Uterine serous carcinoma (USC) is an aggressive subtype of endometrial carcinoma characterized by TP53 mutations ( > 90%), often concomitantly with oncogenic mutations or amplifications that can increase replication stress. As such, USC may therefore be uniquely sensitive to further interference of cell cycle regulation by Wee1 ...
J.F. Liu +12 more
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