LYCOS RETRIEVER 
Aurora: Aurora Kinases
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Aurora kinases (... known as BTAK and STK15) are a family of serine- threonine kinases that have been strongly linked to tumorigenesis. Aurora kinases, which play a central role in controlling cell division, are disregulated in many types of human cancer, including leukemia, colon and breast cancer. Overexpression of Aurora kinase has been shown to promote the transformation of normal cells into cancer cells, and decreased Aurora kinase activity is associated with enhanced function of the body's normal tumor suppressor genes. Amplification of Aurora genes is associated with progression of colorectal cancer and poor prognosis in certain types of breast cancer.
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Aurora kinases are enzymes that play a key role in mitosis, or cell division. They are over-expressed in many human cancers, including breast, colon, pancreas, prostate and thyroid cancer, and are associated with carcinogenesis. Several aurora kinase inhibitors are currently under clinical evaluation for the treatment of cancer.
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VRTX News\r\nhave demonstrated for the first time that a selective small molecule inhibitor\r\nof the Aurora kinases, VX680, profoundly reduces tumor growth in cancer\r\nmodels. Aurora kinases are known to be overexpressed in many tumor types,\r\nincluding colon cancer, breast cancer, and leukemia.\r\nResearch into the function and activity of Aurora kinases over the past\r\nseveral years has suggested that they may play multiple roles in the\r\ndevelopment and progression of cancer, by acting as regulators of cell\r\nproliferation, by transforming normal cells into cancer cells, and by\r\ndownregulating p53, one of the bodys natural tumor suppressors.In the study reported today, the small molecule Aurora kinase inhibitor\r\nVX680 blocked cancer cell proliferation, and ... triggered cell death in a\r\nbroad range of tumor cell types. Data from in vivo xenograft models indicated\r\nthat VX680 achieved complete inhibition of tumor growth at welltolerated\r\ndoses, and in some instances, tumor regression was observed. The report\r\nsuggests that Aurora kinase inhibition provides a promising, novel approach\r\nfor the treatment of multiple human malignancies.Aurora kinases represent a potentially important class of targets for the\r\nfuture treatment of cancer, and we have now demonstrated for the first time\r\nthat a small molecule Aurora kinase inhibitor not only blocks tumor cell\r\nproliferation but also induces tumor cell death, commented Karen Miller,\r\nPh.D., Director of Biology, Vertex Europe and senior author of the study.\r\nThe ability of VX680 to cause tumor regression is particularly exciting.VX680 has demonstrated promising results in a range of tumor types,\r\nsaid Peter Mueller, Ph.D., Chief Scientific Officer of Vertex. Inhibition of\r\nAurora kinases represents a novel and highly targeted approach to cancer\r\ntherapy, and we look forward to the evaluation of Aurora kinase inhibitors in\r\nthe clinic in 2004.Aurora Kinases and CancerAurora kinases also known as BTAK and STK15 are a family of serine\r\nthreonine kinases that have been strongly linked to tumorigenesis. Aurora\r\nkinases, which play a central role in controlling cell division, are\r\ndisregulated in many types of human cancer, including leukemia, colon and\r\nbreast cancer.
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Discovered by Sunesis, SNS-314 is targeted to inhibit Aurora kinases ... halting cell division at the mitotic phase of the cell cycle and blocking the uncontrolled cellular proliferation associated with tumor growth. Aurora kinases have been detected at high levels in tumors from several cancer types, including colon, breast, ovarian, bladder, esophageal, gastric and pancreatic. Sunesis recently filed an Investigational New Drug Application with the U.S. Food and Drug Administration (FDA) for SNS-314 and the company expects to initiate a Phase 1 single-agent clinical trial in patients with advanced solid tumor malignancies in the first half of this year.
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ENMD-2076 is a novel, dual-acting, kinase inhibitor with potent activity against Aurora A and tyrosine kinases linked to promoting cancer and inflammatory diseases. ENMD-2076 acts through multiple pathways resulting in antiproliferative activity and the inhibition of angiogenesis. ENMD-2076 has demonstrated substantial, dose-dependent efficacy as a single agent in multiple xenograft models, including tumor regression in breast, colon, and leukemia models. Importantly, ENMD-2076 is an oral agent that has shown an acceptable toxicity profile in preclinical studies without cardiovascular effects.
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In October 2005, the two companies entered into a worldwide collaboration, excluding Japan, to develop R763/AS703569 and other Aurora kinase inhibitors. As part of this agreement, Merck Serono had the right to add Japan to its territory.
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Aurora Kinases