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极光 A 和 B 激酶——新型抗癌药物的靶点。

Aurora A and B kinases--targets of novel anticancer drugs.

机构信息

Dipartiment of Biology and Cellular and Molecular Pathology, School of Medicine, University of Naples Federico II, via s. Pansini 5, 80131 Napoli, Italy.

出版信息

Recent Pat Anticancer Drug Discov. 2010 Nov;5(3):219-41. doi: 10.2174/157489210791760517.

Abstract

The Aurora Kinases are highly related serine-threonine kinases, essential for accurate and equal segregation of genomic material during mitosis. A large number of studies have linked the aberrant expression of Aurora kinases to cancer, leading to the development of specific Aurora kinases inhibitors. Several small molecules inhibit with a similar efficacy both Aurora A and Aurora B, however, in most cases the effects resemble Aurora B disruption by genetic methods, indicating that Aurora B represents an effective therapeutic target. These drugs are currently under preclinical or clinical evaluation and are reviewed in this article. The relevant patents are discussed.

摘要

极光激酶是高度相关的丝氨酸/苏氨酸激酶,对于有丝分裂过程中基因组物质的准确和均等分离至关重要。大量研究表明,极光激酶的异常表达与癌症有关,从而导致了特定的极光激酶抑制剂的开发。一些小分子以相似的效力抑制极光 A 和极光 B,然而,在大多数情况下,这些效果类似于通过遗传方法破坏极光 B,表明极光 B 是一个有效的治疗靶点。这些药物目前正在进行临床前或临床评估,并在本文中进行了综述。讨论了相关专利。

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