Combining DNA damaging agents and checkpoint 1 inhibitors

Current Medicinal Chemistry. Anti-cancer Agents
Michelle Prudhomme

Abstract

During the cell cycle that leads to mitosis, checkpoints are activated in response to DNA damage. The checkpoints control the ability of cells to arrest the cell cycle allowing time to repair the DNA. In more than 50% of cancer cells, the G1 checkpoint is inactive due to mutations of p53. Therefore, the combination of a DNA damaging agent with a G2 checkpoint inhibitor should force selectively cancer cells into a premature and lethal mitosis. This approach which has recently drawn considerable interest is discussed in this paper.

Citations

Jan 1, 2010·Expert Review of Clinical Pharmacology·Susan Ashwell
Aug 13, 2008·Expert Opinion on Investigational Drugs·Susan AshwellSonya Zabludoff
Mar 7, 2008·Bioorganic & Medicinal Chemistry·Elisabeth ConchonMichelle Prudhomme
Dec 1, 2006·European Journal of Pharmacology·Hélène HénonMichelle Prudhomme
Sep 15, 2007·ChemMedChem·Kenneth L Arrington, Vadim Y Dudkin
Jan 1, 2014·Bioorganicheskaia khimiia·O V GoryunovaN E Kuzmina
Sep 5, 2008·Molecular Pharmacology·Christelle MarminonMichelle Prudhomme
Jul 3, 2008·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Susan Ashwell, Sonya Zabludoff

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Cell cycle checkpoints are a series of complex checkpoint mechanisms that detect DNA abnormalities and ensure that DNA replication and repair are complete before cell division. They are primarily regulated by cyclins, cyclin-dependent kinases, and the anaphase-promoting complex/cyclosome. Here is the latest research.

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