Results 151 to 160 of about 499,052 (176)

WEE1 Kinase As a Target for Cancer Therapy

Journal of Clinical Oncology, 2015
Exploiting the complex machinery that regulates cell cycle checkpointsandDNArepair forcancertherapyhasbeenthefocusofmanypast and ongoing investigations; however, successful translation into patient care and meaningful impact on clinical outcomes have proven elusive. Eukaryotic cells rely on complex cell cycle checkpoint and DNA repair systems to ensure
Sabine, Mueller, Daphne A, Haas-Kogan
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Investigation of biaryl heterocycles as inhibitors of Wee1 kinase

Bioorganic & Medicinal Chemistry Letters, 2019
In 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, Chunqiu, Lai, Maricel, Torrent, Kenneth, Bromberg, Fritz G, Buchanan, Debra, Ferguson, Velitchka, Bontcheva, Eric F, Johnson, Loren, Lasko, David, Maag, Alexander R, Shoemaker, Thomas D, Penning   +11 more
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Nuclear tyrosine kinases: from Abl to WEE1

Current Opinion in Cell Biology, 1996
The notion of a critical role for protein tyrosine kinases in the nucleus is supported by recent findings linking these proteins with components of the cell cycle and with the transcription machinery. Several of these tyrosine kinases localize to both nuclear and cytoplasmic compartments of the cell, and may coordinate signal transduction events in the
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Targeting Wee1-like protein kinase to treat cancer

Drug News & Perspectives, 2010
New anticancer agents are needed in order to overcome the resistance of cancer cells to standard chemotherapy. At present, many of the molecular events that drive the malignant transformation and progression have been identified and there is optimism that the development of agents that specifically target such events will improve treatment outcomes ...
Anastasios, Stathis, Amit, Oza
openaire   +2 more sources

Strategic development of AZD1775, a Wee1 kinase inhibitor, for cancer therapy

Expert Opinion on Investigational Drugs, 2018
Wee1 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, Yu-Dong Wang, Siqing Fu   +2 more
exaly   +3 more sources

The wee1 protein kinase is required for radiation-induced mitotic delay

Nature, 1992
Cellular feedback or 'checkpoint' mechanisms maintain the order of completion of essential, cell-cycle related functions. In the budding yeast, for example, the RAD9 gene product is required to delay progression into mitosis in response to DNA damage. Similarly, in fission yeast, the cdc25 and cdc2 gene products influence the ability of cells to delay ...
R, Rowley, J, Hudson, P G, Young
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Revisiting CHK1 and WEE1 kinases as therapeutic targets in cancer

Biochimica et Biophysica Acta (BBA) - Reviews on Cancer
Uncontrolled cell division is a defining characteristic of cancer, driven by genomic instability. This instability disrupts the DNA damage response network, exacerbates replication stress, and impairs cell cycle checkpoints. Although conventional DNA-damaging therapies like chemotherapy and radiotherapy exploit this vulnerability, they often cause ...
Nehal Arvind, Kumar, P, Manasa, Jaikanth, Chandrasekaran   +2 more
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Myt1: a Wee1-type kinase that phosphorylates Cdc2 on residue Thr14

1997
Most somatic cell division cycles contain a gap period (G2 phase) between the completion of DNA synthesis and the initiation of mitosis. This delay of mitotic entry is controlled, at least in part, by the repression of Cdc2 kinase activity by the phosphorylation of two conserved residues (Thr14 and Tyr15) within the ATP-binding pocket of the Cdc2 ...
A, Fattaey, R N, Booher
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G2 regulatory processes require speedbump for Wee1 kinase activity

Developmental Biology
Wee1 is a conserved Cdk1 inhibitory kinase operating at the G2/M checkpoint to prevent entry into mitosis until the genome has been surveilled and replication is complete. We report here that the early arrest mutant speedbump is a loss-of-function mutation in the zebrafish ortholog of wee1.
Rachel M. Warga, Donald A. Kane
openaire   +2 more sources

Inhibitors of cell cycle checkpoint target Wee1 kinase – a patent review (2003–2022)

Expert Opinion on Therapeutic Patents, 2022
Yadong Chen, Yong Zhu
exaly