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BI811283 : ウィキペディア英語版
BI811283
BI 811283 is a small molecule inhibitor of the Aurora B kinase protein being developed by Boehringer Ingelheim for use as an anti-cancer agent. BI 811283 is currently in the early stages of clinical development and is undergoing first in human trials in patients with solid tumors and Acute Myeloid Leukaemia.
== Mechanism of action ==
BI 811283 is a small molecule drug that selectively binds to the ATP binding pocket of the Aurora B Kinase protein, inhibiting its function in cell division.〔
〕 The Aurora B kinase protein (also known as STK12) is one of a family of proteins that plays an essential role in the alignment, movement and separation of chromosomes during cell division. Aurora B kinase is produced in all dividing cells in normal tissue however; the levels of Aurora B kinase are abnormally raised in many types of cancer.〔
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〕 Abnormally elevated levels of Aurora B kinase, cause unequal chromosomal separation during cell division, resulting in the formation of cells with abnormal numbers of chromosomes, which are both a cause and driver of cancer.
Inhibition of Aurora B kinase by BI 811283 in cancer cells leads to the formation of cells with severely abnormal numbers of chromosomes (polyploid). Counterintuitively, inhibition of Aurora B kinase by BI 811283 actually causes the polyploid cells formed to continue dividing however, because these cells have severe chromosomal abnormalities, they eventually stop dividing or undergo cell death.〔

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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