Department of Chemistry, Lakehead University, 955 Oliver Road, Thunder Bay, ON P7B 5E1, Canada.
Thunder Bay Regional Health Research Institute, 980 Oliver Road, Thunder Bay, ON P7B 6V4, Canada.
Molecules. 2023 Apr 11;28(8):3385. doi: 10.3390/molecules28083385.
The Aurora kinases (A, B, and C) are a family of three isoform serine/threonine kinases that regulate mitosis and meiosis. The Chromosomal Passenger Complex (CPC), which contains Aurora B as an enzymatic component, plays a critical role in cell division. Aurora B in the CPC ensures faithful chromosome segregation and promotes the correct biorientation of chromosomes on the mitotic spindle. Aurora B overexpression has been observed in several human cancers and has been associated with a poor prognosis for cancer patients. Targeting Aurora B with inhibitors is a promising therapeutic strategy for cancer treatment. In the past decade, Aurora B inhibitors have been extensively pursued in both academia and industry. This paper presents a comprehensive review of the preclinical and clinical candidates of Aurora B inhibitors as potential anticancer drugs. The recent advances in the field of Aurora B inhibitor development will be highlighted, and the binding interactions between Aurora B and inhibitors based on crystal structures will be presented and discussed to provide insights for the future design of more selective Aurora B inhibitors.
极光激酶（A、B 和 C）是一个家族的三种同工型丝氨酸/苏氨酸激酶，调节有丝分裂和减数分裂。包含极光 B 作为酶成分的染色体乘客复合物（CPC）在细胞分裂中起着关键作用。CPC 中的极光 B 确保了染色体的正确分离，并促进了有丝分裂纺锤体上染色体的正确取向。在几种人类癌症中观察到极光 B 的过表达，并与癌症患者的预后不良有关。用抑制剂靶向极光 B 是癌症治疗的一种有前途的治疗策略。在过去的十年中，学术界和工业界都广泛地研究了极光 B 抑制剂作为潜在的抗癌药物。本文对极光 B 抑制剂的临床前和临床候选药物作为潜在的抗癌药物进行了全面综述。将重点介绍极光 B 抑制剂开发领域的最新进展，并根据晶体结构展示和讨论极光 B 与抑制剂之间的结合相互作用，为未来设计更具选择性的极光 B 抑制剂提供见解。
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