Dipartiment of Biology and Cellular and Molecular Pathology, School of Medicine, University of Naples Federico II, via s. Pansini 5, 80131 Napoli, Italy.
Recent Pat Anticancer Drug Discov. 2010 Nov;5(3):219-41. doi: 10.2174/157489210791760517.
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.
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。