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Molecular Properties:
- Chemical Structure: GSK461364 is a small-molecule inhibitor designed to target and disrupt the function of Eg5, which is involved in the formation of the mitotic spindle during cell division. Its structure allows it to specifically bind to the ATPase motor domain of Eg5, blocking its motor activity and preventing the correct positioning of the spindle poles.
- Mechanism of Action: GSK461364 specifically inhibits the ATP-dependent motor function of Eg5, preventing the proper separation of the mitotic spindle during mitosis. Eg5 is crucial for the formation of bipolar spindles, which are necessary for the equal segregation of chromosomes during cell division. By inhibiting Eg5, GSK461364 causes cells to accumulate in mitosis and ultimately undergo apoptosis due to failed mitotic progression.
- Selective Inhibition: Unlike other mitotic inhibitors that may affect a broad range of cellular processes, GSK461364 is a selective inhibitor of Eg5, making it a valuable tool for studying this particular protein and its role in cell division. Its specificity helps minimize off-target effects, allowing for more accurate experimental results.
Research Use in Cancer Therapy:
GSK461364’s ability to arrest cells in mitosis makes it a promising candidate in the treatment of various cancers, particularly those with a high rate of cell division. By targeting Eg5, GSK461364 selectively impacts rapidly dividing cancer cells, while potentially sparing non-dividing cells, thus providing an effective treatment strategy. Its role in combination therapies offers hope for improving treatment outcomes, especially in tumors resistant to conventional chemotherapy.
In summary, GSK461364 is a valuable tool for studying mitotic cell division, with significant implications in cancer research and therapeutic development. It provides insight into the role of Eg5 in cell division and holds potential as an anti-cancer agent, both on its own and in combination with other treatments.