Most human cancer cells are characterized by changes in the amount or organization of DNA resulting in chromosome instability and aneuploidy Several mitotic kinases, Aurora kinases amongst others, regulate the progression of the cell through mitosis So far three Aurora kinases have been identified in man: Aurora-A, Aurora-B and Aurora-C Aurora kinases were recently identified as a potential target in anticancer therapy, and various Aurora-A and Aurora-B kinase inhibitors are in development In this review we provide a brief insight into the mechanism of action as far as currently available We review the available pre-clinical data, discuss the clinical phase I data and try to give a direction for future headings

Aurora kinase inhibitors

http://csmres.co.uk/cs.public.upd/article-downloads/2011_2-63407.pdf

Aurora-A kinase inhibitor scaffolds and binding modes.

Tubulin is a very important target for cancer-fighting therapies; therefore, the cancer research community continues to adopt new ways of developing the therapeutic potential of tubulin and tubulin-associated proteins. Two families of tubulin-associated kinases, Aurora and Polo-like, have received significant attention regarding how they contribute to tumorigenesis and can be targeted with selective small molecule inhibitors. Aurora and Polo-like kinases play essential roles in centrosome separation, chromosome alignment and segregation, and cytokinesis. Inhibition of any of these kinases results in abnormal mitotic events (which vary depending on the particular family member) and eventually leads to apoptosis. Because of the biological consequences of inhibiting these kinases, several Aurora or Polo-like selective inhibitors have advanced to various stages of preclinical and clinical development; the most advanced are currently in phase 2 clinical trials.

Tubulin-associated proteins: Aurora and Polo-like kinases as therapeutic targets in cancer.

Background: Although cellular immunotherapy still remains in its infancy, it is one of the important treatment options against cancer. The marked improvement of its clinical efficacy requires a ‘better’ target antigen, which is well recognized by cancer-cell-specific cytotoxic T lymphocytes. We have recently demonstrated the potential of Aurora-A kinase (Aurora-A) as such a ‘better’ target for cellular immunotherapy against human leukemia. Aurora-A is a member of the serine/threonine kinase family that properly regulates the cell division process, and has recently been implicated in tumorigenesis. On the other hand, small-molecule inhibitors targeting Aurora-A have recently been developed and preliminary but promising observations from Phase I clinical trials have been reported. These facts highlight the attractiveness of Aurora-A as an important target of comprehensive cancer therapies. Objective/methods: In this review, we cover Aurora-A in the areas of immunotherapy and small-molecule inhibitor therapy...

Aurora-A kinase: a novel target both for cellular immunotherapy and molecular target therapy against human leukemia.

Cancers of the stomach, gastroesophageal junction and esophagus are a major cause of cancer-related deaths worldwide. In Western countries, adenocarcinomas of the distal esophagus, gastroesophageal junction and proximal stomach have been increasing in frequency more rapidly than other malignancies. The majority of newly diagnosed patients present with advanced disease and the overall survival remains dismal at approximately 10% at 5 years. Better understanding of tumor biology has led to the development of promising novel therapeutic strategies. There is therefore increasing optimism that some of these approaches will improve the outcomes in these increasingly common cancers. Given the success of antiangiogenesis as a therapeutic strategy in various types of cancer, there are ongoing efforts to investigate the utility of other targeted therapies in the treatment of gastric and esophageal cancers. This review will focus on novel therapeutic targets other than angiogenesis and provide a rationale for the further clinical evaluation of these agents in patients with upper gastrointestinal tract cancers.

Novel targets in esophageal and gastric cancer: beyond antiangiogenesis

3577 Background: MLN8054 is a small molecule inhibitor of Aurora A kinase, with > 150-fold greater potency against this enzyme than the structurally related but functionally distinct Aurora B kinas...

Phase I clinical trial of MLN8054, a selective inhibitor of Aurora A kinase

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Phase I clinical trial of MLN8054, a selective inhibitor of Aurora A kinase