Results 111 to 120 of about 677,925 (163)
WEE1 Kinase Inhibitor Shows Promise [PDF]
Nature Reviews Clinical Oncology, 2019 Peter Sidaway
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Clinical Development of WEE1 Inhibitors in Gynecological Cancers: A Systematic Review
Cancer Treatment Reviews, 2023 Introduction: The anti-tumor activity of WEE1 inhibitors (WEE1i) in gynecological malignancies has recently been demonstrated in clinical trials and its rationale is based on biological/molecular features of gynecological cancers. With this systematic review, we aim to outline the clinical development and current evidence regarding the efficacy and ...
Tim Schutte +2 more
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Structure-Activity Relationships of Wee1 Inhibitors: A Review
European Journal of Medicinal Chemistry, 2020Wee1 kinase plays an important role in regulating G2/M checkpoint and S phase, and the inhibition of it will lead to mitotic catastrophe in cancer cells with p53 mutation or deletion. Therefore, the mechanism of Wee1 kinase in cancer treatment and the development of its inhibitors have become a research hotspot.
Jun He, Jianyou Shi, Yiwen Zhang
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Selective Wee1 Inhibitors Led to Antitumor Activity in Vitro and Correlated With Myelosuppression
ACS Medicinal Chemistry Letters, 2023 [Image: see text] Wee1 is a tyrosine kinase that is highly expressed in several cancer types. Wee1 inhibition can lead to suppression of tumor cell proliferation and sensitization of cells to the effects of DNA-damaging agents.
Christopher Jones +2 more
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Pediatric DDR inhibitor combinations: Are WEE1 there yet?
Cancer, 2023A phase 2 study of the WEE1 inhibitor adavosertib in combination with irinotecan in children demonstrates an intriguing positive signal of efficacy in neuroblastoma, a pediatric tumor characterized by replication stress. Further pediatric development of adavosertib and related compounds targeting DNA damage response will be challenged by appropriate ...
Emily K. Slotkin +2 more
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Investigation of biaryl heterocycles as inhibitors of Wee1 kinase
Bioorganic & Medicinal Chemistry Letters, 2019In continuation of our previous research towards the discovery of potent, selective and drug-like Wee1 inhibitors, 2 novel series of biaryl heterocycles were designed, synthesized and evaluated. The new biaryl cores were designed to enable structure-activity exploration of substituents at C-8 or N-8 which were used for tuning compound properties and to
Anthony, Mastracchio +11 more
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Uterine Serous Carcinoma Responds to the WEE1 Inhibitor Adavosertib
Cancer Discovery, 2021Abstract The overall response rate to adavosertib was 29.4%; no biomarkers predicting response were found.
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Discovery of pyrido[4,3-d]pyrimidinone derivatives as novel Wee1 inhibitors
Bioorganic & Medicinal Chemistry, 2023Wee1 has emerged as a potential target in cancer therapy due to its critical role in the regulation of the cell cycle. Here, we describe a series of Wee1 inhibitors with a novel scaffold that are potent inhibitors of this kinase (IC50 = 19-1485 nM). These inhibitors demonstrated robust cytotoxicity in MV-4-11 and T47D cell lines (MV-4-11 IC50 = 660 ...
Qingqing Ye +7 more
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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 ...
Siqing, Fu +4 more
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Adavosertib and beyond: Biomarkers, drug combination and toxicity of WEE1 inhibitors
Critical Reviews in Oncology/HematologyWEE1 kinase is renowned as an S-G2 checkpoint inhibitor activated by ATR-CHK1 in response to replication stress. WEE1 inhibition enhances replication stress and effectively circumvents checkpoints into mitosis, which triggers significant genetic impairs and culminates in cell death.
Chi, Zhang +4 more
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