A new drug that blocks cancer's escape route from chemotherapy could be used to treat deadly lung and pancreatic cancers, new research reports. Scientists have shown in human cancer cells and in mice that the drug, which was discovered at The Institute of Cancer Research in London, boosts the effectiveness of conventional chemotherapy. The drug, known as CCT245737, is scheduled to begin first-in-human clinical trials in patients with lung and pancreatic cancers - two cancers with low survival rates that continue to resist currently available treatments. CCT245737 is the first orally active, clinical development candidate CHK1 inhibitor to be described. The new study was published online on July 22, 2015 the journal Oncotarget, and was funded by Cancer Research UK and Sareum Limited. The article is titled “The Clinical Development Candidate CCT245737 Is an Orally Active CHK1 Inhibitor with Preclinical Activity in RAS Mutant NSCLC and Eµ-MYC Driven B-cell Lymphoma.” The research, conducted at The Institute of Cancer Research (ICR) in collaboration with colleagues at the drug discovery company Sareum and at Newcastle University, shows the effectiveness of a new class of drugs called CHK1 inhibitors that can be delivered orally to patients. Most chemotherapies work by damaging the DNA of rapidly dividing cells. But in response, cancer cells activate a molecule called CHK1 that delays cell division and gives cancer cells time to repair their damaged DNA. Scientists hoped that blocking CHK1 could stop cancer cells from repairing DNA damage and prevent them from becoming resistant to the cell-killing effects of chemotherapy. Researchers developed techniques to assess the method of action of CCT245737 in human cancer cell lines, and demonstrated that it potently blocked the molecule CHK1.
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