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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.

DOI:10.2174/157489210791760517
PMID:20524930
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。

相似文献

1
Aurora A and B kinases--targets of novel anticancer drugs.极光 A 和 B 激酶——新型抗癌药物的靶点。
Recent Pat Anticancer Drug Discov. 2010 Nov;5(3):219-41. doi: 10.2174/157489210791760517.
2
Aurora-B kinase inhibitors for cancer chemotherapy.用于癌症化疗的极光激酶B抑制剂。
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Aurora kinase inhibitors as anticancer molecules.极光激酶抑制剂作为抗癌分子。
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Aurora kinases: new targets for cancer therapy.极光激酶:癌症治疗的新靶点。
Clin Cancer Res. 2006 Dec 1;12(23):6869-75. doi: 10.1158/1078-0432.CCR-06-1405.
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Targeting aurora kinases in cancer treatment.在癌症治疗中靶向极光激酶。
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Aurora kinase inhibitors: a new class of drugs targeting the regulatory mitotic system.极光激酶抑制剂:靶向调控有丝分裂系统的新型药物。
Clin Transl Oncol. 2009 Dec;11(12):787-98. doi: 10.1007/s12094-009-0447-2.
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Update on aurora kinase inhibitors in gynecologic malignancies.妇科恶性肿瘤中极光激酶抑制剂的最新进展
Recent Pat Anticancer Drug Discov. 2008 Nov;3(3):162-77. doi: 10.2174/157489208786242322.
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Aurora kinase inhibitors: progress towards the clinic.极光激酶抑制剂:向临床应用迈进。
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Aurora kinase inhibitors as anti-cancer therapy.极光激酶抑制剂作为抗癌疗法。
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Target validation and biomarker identification in oncology : the example of aurora kinases.肿瘤学中的靶点验证与生物标志物鉴定:以极光激酶为例
Mol Diagn Ther. 2008;12(2):71-6. doi: 10.1007/BF03256272.

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Specificity rendering 'hot-spots' for aurora kinase inhibitor design: the role of non-covalent interactions and conformational transitions.用于极光激酶抑制剂设计的特异性呈现“热点”:非共价相互作用和构象转变的作用
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Gene expression of Aurora kinases in prostate cancer and nodular hyperplasia tissues.前列腺癌和结节性增生组织中 Aurora 激酶的基因表达。
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Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.开发邻氯苯基取代嘧啶作为极其有效的极光激酶抑制剂。
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